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Daniela G. Dengler, Qing Sun, John Holleran, Sirkku Pollari, Jannis Beutel, Brock T. Brown, Aki Shinoki Iwaya, Robert Ardecky, Kaleeckal G. Harikumar, Laurence J. Miller, Eduard A. Sergienko | Development of a Testing Funnel for Identification of Small Molecule Modulators Targeting Secretin Receptors | SLAS Discov. 2021 Jan; 26(1): 1-16. |
Dominik Loser, Jasmin Schaefer, Timm Danker, Clemens Moller, Markus Brull, Ilinca Suciu, Anna-Katharina Uckert, Stefanie Klima, Marcel Leist, Udo Kraushaar | Human neuronal signaling and communication assays to assess functional neurotoxicity | Arch Toxicol. 2021; 95(1): 229-252. |
Tianshu Xiao, Jianming Lu, Jun Zhang, Rebecca I. Johnson, Lindsay G.A. McKay, Nadia Storm, Christy L. Lavine, Hanqin Peng, Yongfei Cai, Sophia Rits-Volloch, Shen Lu, Brian D. Quinlan, Michael Farzan, Michael S. Seaman, Anthony Griffiths, Bing Chen | A trimeric human angiotensin-converting enzyme 2 as an anti-SARS-CoV-2 agent | Nat Struct Mol Biol. 2021 Feb; 28(2): 202-209. |
Jun Li, Jong-Kook Lee, Keiko Miwa, Yuki Kuramoto, Kiyoshi Masuyama, Hideki Yasutake, Satoki Tomoyama, Hiroyuki Nakanishi, Yasushi Sakata | Scaffold-Mediated Developmental Effects on Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes Are Preserved After External Support Removal | Front Cell Dev Biol. 2021; 9: 591754. |
Nicole M. Fisher, Aqeela AlHashim, Aditi B. Buch, Hana Badivuku, Manar M. Samman, Kelly M. Weiss, Gabriela I. Cestero, Mark D. Does, Jerri M. Rook, Craig W. Lindsley, P. Jeffrey Conn, Rocco G. Gogliotti, Colleen M. Niswender | A GRM7 mutation associated with developmental delay reduces mGlu7 expression and produces neurological phenotypes | JCI Insight. 2021 Feb 22; 6(4): e143324. |
Kambiz Shekdar, Jessica Langer, Srinivasan Venkatachalan, Lori Schmid, Jonathan Anobile, Purvi Shah, Amy Lancaster, Olga Babich, Olga Dedova, Dennis Sawchuk | Cell engineering method using fluorogenic oligonucleotide signaling probes and flow cytometry | Biotechnol Lett. 2021 Mar 8 : 1-10. |
Aurelia C. Balestra, Konstantinos Koussis, Natacha Klages, Steven A. Howell, Helen R. Flynn, Marcus Bantscheff, Carla Pasquarello, Abigail J. Perrin, Lorenzo Brusini, Patrizia Arboit, Olalla Sanz, Laura Peces-Barba Castano, Chrislaine Withers-Martinez, Alexandre Hainard, Sonja Ghidelli-Disse, Ambrosius P. Snijders, David A. Baker, Michael J. Blackman, Mathieu Brochet | Ca2+ signals critical for egress and gametogenesis in malaria parasites depend on a multipass membrane protein that interacts with PKG | Sci Adv. 2021 Mar; 7(13): eabe5396. |
Dominik Loser, Maria G. Hinojosa, Jonathan Blum, Jasmin Schaefer, Markus Brull, Ylva Johansson, Ilinca Suciu, Karin Grillberger, Timm Danker, Clemens Moller, Iain Gardner, Gerhard F. Ecker, Susanne H. Bennekou, Anna Forsby, Udo Kraushaar, Marcel Leist | Functional alterations by a subgroup of neonicotinoid pesticides in human dopaminergic neurons | Arch Toxicol. 2021; 95(6): 2081-2107. |
Tomoya Uchimura, Toshifumi Asano, Takao Nakata, Akitsu Hotta, Hidetoshi Sakurai | A muscle fatigue-like contractile decline was recapitulated using skeletal myotubes from Duchenne muscular dystrophy patient-derived iPSCs | Cell Rep Med. 2021 Jun 15; 2(6): 100298. |
Polina Isaikina, Ching-Ju Tsai, Nikolaus Dietz, Filip Pamula, Anne Grahl, Kenneth N. Goldie, Ramon Guixa-Gonzalez, Camila Branco, Marianne Paolini-Bertrand, Nicolas Calo, Fabrice Cerini, Gebhard F. X. Schertler, Oliver Hartley, Henning Stahlberg, Timm Maier, Xavier Deupi, Stephan Grzesiek | Structural basis of the activation of the CC chemokine receptor 5 by a chemokine agonist | Sci Adv. 2021 Jun; 7(25): eabg8685. |
Masahiko Soga, Takaya Izumi, Isamu Nanchi, Narumi Horita, Miyuki Yamamoto, Shiori Kawasaki, Koichi Ogawa, Masahide Fujita, and Yasuhide Morioka | Suppression of joint pain in transient receptor potential vanilloid 4 knockout rats with monoiodoacetate-induced osteoarthritis | Pain Rep. 2021 Sep-Oct; 6(3): e951. |
Shiori Kawasaki, Masahiko Soga, Yusuke Sakurai, Isamu Nanchi, Miyuki Yamamoto, Sunao Imai, Tatsuya Takahashi Naoki Tsuno, Toshiyuki Asaki, Yasuhide Morioka, Masahide Fujita | Selective blockade of transient receptor potential vanilloid 4 reduces cyclophosphamide-induced bladder pain in mice | European Journal of Pharmacology Volume 899, 15 May 2021, 174040 |
Naoki Aizawa, Yoshikazu Fujimori, Osamu Nakanishi, Takemitsu Hayashi, Yoshiaki Goi, Jun-ichi Kobayashi, Tomoe Fujita | Efficacy of the combination of KPR-5714, a novel transient receptor potential melastatin 8 (TRPM8) antagonist, and β3-adrenoceptor agonist or anticholinergic agent on bladder dysfunction in rats with bladder overactivity | European Journal of Pharmacology Volume 899, 15 May 2021, 173995 |
Magdalene M Moran, Bertrand L Chenard, Timothy Strassmaier | Treatment with HC-070, a Potent Inhibitor of TRPC4 and TRPC5, Leads to Anxiolytic and Antidepressant Effects in Mice | Single Cell Biology |
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Wayne Childers, Rong Fan, Rogelio Martinez, Dennis J. Colussi, Edward Melenski, Yuxiao Liu, John Gordon, Magid Abou-Gharbia, Marlene A. Jacobson | Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells | Bioorg Med Chem Lett. 2020 Jan 15; 30(2): 126806. |
Hiroyuki Ogasawara, Masahiro Furuno, Koji Edamura, Masato Noguchi | Peptides of major basic protein and eosinophil cationic protein activate human mast cells | Biochem Biophys Rep. 2020 Mar; 21: 100719. |
Francis Rousset, German Nacher-Soler, Marta Coelho, Sten Ilmjarv, Vivianne Beatrix Christina Kokje, Antoine Marteyn, Yves Cambet, Michael Perny, Marta Roccio, Vincent Jaquet, Pascal Senn, and Karl Heinz Krause | Redox activation of excitatory pathways in auditory neurons as mechanism of age-related hearing loss | Redox Biol. 2020 Feb; 30: 101434. |
Marta Sanchez-Soto, Ravi Kumar Verma, Blair K.A. Willette, Elizabeth C. Gonye, Annah M. Moore, Amy E. Moritz, Comfort A. Boateng, Hideaki Yano, R. Benjamin Free, Lei Shi, David R. Sibley | A structural basis for how ligand binding site changes can allosterically regulate GPCR signaling and engender functional selectivity | Sci Signal. 2020 Feb 4; 13(617): eaaw5885. |
Sayuri Suzuki, Reinhold Penner, Andrea Fleig | TRPM7 contributes to progressive nephropathy | Sci Rep. 2020; 10: 2333. |
Giulia Di Marco, Francesca Vallese, Benjamin Jourde, Christian Bergsdorf, Mattia Sturlese, Agnese De Mario, Valerie Techer-Etienne, Dorothea Haasen, Berndt Oberhauser, Simone Schleeger, Giulia Minetti, Stefano Moro, Rosario Rizzuto, Diego De Stefani, Mara Fornaro, Cristina Mammucari | A High-Throughput Screening Identifies MICU1 Targeting Compounds | Cell Rep. 2020 Feb 18; 30(7): 2321-2331.e6. |
Tianyu Wang, Shumpei Nakagawa, Takahito Miyake, Genzui Setsu, Sumihiro Kunisue, Kaoru Goto, Akira Hirasawa, Hitoshi Okamura, Yoshiaki Yamaguchi, Masao Doi | Identification and functional characterisation of N-linked glycosylation of the orphan G protein-coupled receptor Gpr176 | Sci Rep. 2020; 10: 4429. |
Martin Kriebel, Julia Ebel, Florian Battke, Stefan Griesbach, and Hansjurgen Volkmer | Interference With Complex IV as a Model of Age-Related Decline in Synaptic Connectivity | Front Mol Neurosci. 2020; 13: 43. |
Shunsuke Maehara, Natsuko Yuge, Chika Higashi, Takumi Ota, Junji Furukawa, Takashi Takeuchi | Pharmacological characterization of a novel potent, selective, and orally active orexin 2 receptor antagonist, SDM‐878 | Neuropsychopharmacol Rep. 2020 Jun; 40(2): 182-189. |
Amy E. Moritz, R. Benjamin Free, Warren S. Weiner, Emmanuel O. Akano, Disha Gandhi, Ara Abramyan, Thomas M. Keck, Marc Ferrer, Xin Hu, Noel Southall, Joseph Steiner, Jeffrey Aube, Lei Shi, Kevin J. Frankowski, David R. Sibley | Discovery, Optimization and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist | J Med Chem. 2020 May 28; 63(10): 5526-5567. |
Ruslana Bryk, Shashirekha Mundhra, Xiuju Jiang, Madeleine Wood, Daniel Pfau, Elaina Weber, Suna Park, Li Zhang, Colin Wilson, Renier Van der Westhuyzen, Leslie Street, Kelly Chibale, Matthew Zimmerman, Veronique Dartois, Nunzia Pastore, Andrea Ballabio, Natalie Hawryluk, Stacie Canan, Vikram Khetani, Joseph Camardo, Carl Nathan, | Potentiation of rifampin activity in a mouse model of tuberculosis by activation of host transcription factor EB | PLoS Pathog. 2020 Jun; 16(6): e1008567. |
Yue Fu, David Estoppey, Silvio Roggo, Dominik Pistorius, Florian Fuchs, Christian Studer, Ashraf S. Ibrahim, Thomas Aust, Frederic Grandjean, Manuel Mihalic, Klaus Memmert, Vivian Prindle, Etienne Richard, Ralph Riedl, Sven Schuierer, Eric Weber, Jurg Hunziker, Frank Petersen, Jianshi Tao, Dominic Hoepfner | Jawsamycin exhibits in vivo antifungal properties by inhibiting Spt14/Gpi3-mediated biosynthesis of glycosylphosphatidylinositol | Nat Commun. 2020; 11: 3387. |
Xiaofei Zhang, Yiding Zhang, Zhen Chen, Tuo Shao, Richard Van, Katsushi Kumata, Xiaoyun Deng, Hualong Fu, Tomoteru Yamasaki, Jian Rong, Kuan Hu, Akiko Hatori, Lin Xie, Qingzhen Yu, Weijian Ye, Hao Xu, Douglas J. Sheffler, Nicholas D. P. Cosford, Yihan Shao, Pingping Tang, Lu Wang, Ming-Rong Zhang, Steven H. Liang | Synthesis and preliminary studies of 11C-labeled tetrahydro-1,7-naphthyridine-2-carboxamides for PET imaging of metabotropic glutamate receptor 2 | Theranostics. 2020; 10(24): 11178-11196. |
Khairunnisa Mentari Semesta, Ruilin Tian, Martin Kampmann, Mark von Zastrow, Nikoleta G. Tsvetanova | A high-throughput CRISPR interference screen for dissecting functional regulators of GPCR/cAMP signaling | PLoS Genet. 2020 Oct; 16(10): e1009103. |
Xiaowei Hou, Ian R Outhwaite, Leanne Pedi, Stephen Barstow Long | Cryo-EM structure of the calcium release-activated calcium channel Orai in an open conformation | eLife. 2020; 9: e62772. |
Francis Rousset, Vivianne B. C. Kokje, Rebecca Sipione, Dominik Schmidbauer, German Nacher-Soler, Sten Ilmjarv, Marta Coelho, Stefan Fink, Francois Voruz, Antoun El Chemaly, Antoine Marteyn, Hubert Lowenheim, Karl-Heinz Krause, Marcus Muller, Rudolf Gluckert, Pascal Senn | Intrinsically Self-renewing Neuroprogenitors From the A/J Mouse Spiral Ganglion as Virtually Unlimited Source of Mature Auditory Neurons | Front Cell Neurosci. 2020; 14: 395. |
Juliette Duchesne De Lamotte, Sylvain Roqueviere, Helene Gautier, Elsa Raban, Celine Boure, Elena Fonfria, Johannes Krupp, Camille Nicoleau | hiPSC-Derived Neurons Provide a Robust and Physiologically Relevant In Vitro Platform to Test Botulinum Neurotoxins | Front Pharmacol. 2020; 11: 617867. |
Stephane Bedut, Ralf Kettenhofen, Jean-Marc D'Angelo | Voltage-sensing optical recording: A method of choice for high-throughput assessment of cardiotropic effects | J Pharmacol Toxicol Methods . 2020 Sep;105:106888. |
Takahiro Yamazaki, Chika Takahashi, Yoshimasa Taniguchi, Masataka Narukawa, Takumi Misaka, Yasuhisa Ano | Bitter taste receptor activation by hop-derived bitter components induces gastrointestinal hormone production in enteroendocrine cells | Biochemical and Biophysical Research Communications Volume 533, Issue 4, 17 December 2020, Pages 704-709 |
Michael K. Pugsley Bisrat Bekele, Helene Griessel, Tessade Korte, Simon Authier, Anne F.Grobler, Carrie G.Markgraf, Michael J.Curtis | Twenty years of safety pharmacology model validation and the wider implications of this to drug discovery | Journal of Pharmacological and Toxicological Methods Volume 105, September 2020, 106912 |
David Reiner Aleksandra Zivkovic, Olivier Labeeuw, Stephane Krief, Marc Capet, Holger Stark | Novel pyrrolidinone derivative lacks claimed histamine H3 receptor stimulation in receptor binding and functional studies | European Journal of Medicinal Chemistry Volume 191, 1 April 2020, 112150 |
Ayako Yoshida, Kouhei Takashima, Tomokazu Shimonaga, Michinori Kadokura, Shotaro Nagase, Shuichi Koda | Establishment of a simple one-step method for oligodendrocyte progenitor cell preparation from rodent brains | Journal of Neuroscience Methods Volume 342, 1 August 2020, 108798 |
Maxime Jacoupy, Emeline Hamon-Keromen | Monitoring the Mitochondrial Presequence Import Pathway In Living Mammalian Cells with a New Molecular Biosensor | Mitochondrial Medicine pp 441-452 |
Takasuna, Kiyoshi, Kazusa, Katsuyuki,Hayakawa Tomohiro | Comprehensive Cardiac Safety Assessment using hiPS-cardiomyocytes (Consortium for Safety Assessment using Human iPS Cells: CSAHi) | Current Pharmaceutical Biotechnology, Volume 21, Number 9, 2020, pp. 829-841(13) |
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Dennis J. Colussi, Marlene A. Jacobson | Patient-Derived Phenotypic High-Throughput Assay to Identify Small Molecules Restoring Lysosomal Function in Tay-Sachs Disease | SLAS Discov. 2019 Mar;24(3):295-303. doi: 10.1177/2472555218814538. Epub 2019 Jan 7. |
Laura B. Duvall, Lavoisier Ramos-Espiritu, Kyrollos E. Barsoum, J. Fraser Glickman, and Leslie B. Vosshall | Small-Molecule Agonists of Ae. aegypti Neuropeptide Y Receptor Block Mosquito Biting | CELL Volume 176, ISSUE 4, P687-701.e5, February 07, 2019 |
Soon-Hee Kim, Misun Seo1, Hongik Hwang1, Dong-Min Moon, Gi Hoon Son, Kyungjin Kim and Hyewhon Rhim | Physical and Functional Interaction between 5-HT6 Receptor and Nova-1 | Exp Neurobiol. 2019 Feb; 28(1): 17-29. |
Akiko Koto, Naoto Motoyama, Hiroki Tahara, Sean McGregor, Minoru Moriyama, Takayoshi Okabe, Masayuki Miura, and Laurent Keller | Oxytocin/vasopressin-like peptide inotocin regulates cuticular hydrocarbon synthesis and water balancing in ants | Proc Natl Acad Sci U S A. 2019 Mar 19; 116(12): 5597-5606. |
Thomas M Keck, R. Benjamin Free, Marilyn M Day, Sonvia L Brown, Michele S Maddaluna, Griffin Fountain, Charles Cooper, Brooke Fallon, Matthew Holmes, Christopher Stang, Russell Burkhardt, Alessandro Bonifazi, Michael P Ellenberger, Amy Hauck Newman, David R. Sibley, Chun Wu, and Comfort A. Boateng | Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy | J Med Chem. 2019 Apr 11; 62(7): 3722-3740. |
Woo Seung Son, Kyu-Sung Jeong, Sang Min Lim, Ae Nim Pae | Structural hybridization of pyrrolidine-based T-type calcium channel inhibitors and exploration of their analgesic effects in a neuropathic pain model | Bioorg Med Chem Lett. 2019 May 15;29(10):1168-1172. doi: 10.1016/j.bmcl.2019.03.026. Epub 2019 Mar 21. |
Koki Yamamoto, Shinsuke Inuki, Hiroaki Ohno, Shinya Oishi | Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact | Bioorg Med Chem Lett. 2019 May 15;27(10):2019-2026. doi: 10.1016/j.bmcl.2019.03.059. Epub 2019 Apr 1. |
Huan Wang, Robert P. Sheehan, Adam C. Palmer, Robert A. Everley, Sarah A. Boswell, Noga Ron-Harel, Alison E. Ringel, Kristina M. Holton, Connor A. Jacobson, Alison R. Erickson, Laura Maliszewski, Marcia C. Haigis, Peter K. Sorger | Adaptation of human iPSC-derived cardiomyocytes to tyrosine kinase inhibitors reduces acute cardiotoxicity via metabolic reprogramming | Cell Syst. 2019 May 22; 8(5): 412-426.e7. |
Haoyu Zeng, Jixin Wang, Holly Clouse, Armando Lagrutta, Frederick Sannajust | Human-induced pluripotent stem cell-derived cardiomyocytes have limited IKs for repolarization reserve as revealed by specific KCNQ1/KCNE1 blocker | JRSM Cardiovasc Dis. 2019 Jan-Dec; 8: 2048004019854919. |
Tevye Jason Stachniak, Emily Lauren Sylwestrak, Peter Scheiffele, Benjamin J. Hall, Anirvan Ghosh | Elfn1-Induced Constitutive Activation of mGluR7 Determines Frequency-Dependent Recruitment of Somatostatin Interneurons | J Neurosci. 2019 Jun 5; 39(23): 4461-4474. |
Zhuo Yang, Yue Wan, Pingdong Tao, Min Qiang, Xue Dong, Chih-Wei Lin, Guang Yang, Tianqing Zheng, Richard A. Lernera | A cell-cell interaction format for selection of high-affinity antibodies to membrane proteins | Proc Natl Acad Sci U S A. 2019 Jul 23; 116(30): 14971-14978. |
Rebekka Wegmann, Marilisa Neri, Sven Schuierer, Bilada Bilican, Huyen Hartkopf, Florian Nigsch, Felipa Mapa, Annick Waldt, Rachel Cuttat, Max R. Salick, Joe Raymond, Ajamete Kaykas, Guglielmo Roma, Caroline Gubser Keller | CellSIUS provides sensitive and specific detection of rare cell populations from complex single-cell RNA-seq data | Genome Biol. 2019; 20: 142. |
Matthew J. Birket, Sophie Raibaud, Miriam Lettieri, Antony D. Adamson, Valerie Letang, Pauline Cervello, Nicolas Redon, Gwenaelle Ret, Sandra Viale, Bing Wang, Bruno Biton, Jean-Claude Guillemot, Vincent Mikol, John P. Leonard, Neil A. Hanley, Cecile Orsini, Jean-Michel Itier | A Human Stem Cell Model of Fabry Disease Implicates LIMP-2 Accumulation in Cardiomyocyte Pathology | Stem Cell Reports. 2019 Aug 13; 13(2): 380-393. |
M. Jacoupy, Hamon-Keromen, A. Ordureau, Z. Erpapazoglou, F. Coge, J.-C. Corvol, O. Nosjean, C. Mannoury la Cour, M. J. Millan, J. A. Boutin, J. W. Harper, A. Brice, D. Guedin, C. A. Gautier, O. Corti | The PINK1 kinase-driven ubiquitin ligase Parkin promotes mitochondrial protein import through the presequence pathway in living cells | Sci Rep. 2019; 9: 11829. |
Chuang-Yu Lin, Michiko Yoshida, Li-Tzu Li, Akihiro Ikenaka, Shiori Oshima, Kazuhiro Nakagawa, Hidetoshi Sakurai, Eriko Matsui, Tatsutoshi Nakahata, Megumu K. Saito | iPSC-derived functional human neuromuscular junctions model the pathophysiology of neuromuscular diseases | JCI Insight. 2019 Sep 19; 4(18): e124299. |
Aderonke Sofoluwe, Marc Bacchetta, Mehdi Badaoui, Brenda R. Kwak, Marc Chanson | ATP amplifies NADPH-dependent and -independent neutrophil extracellular trap formation | Sci Rep. 2019; 9: 16556. |
Mark Gallant Fulton, Matthew Thomas Loch, Caroline Anne Cuoco, Alice Lambert Rodriguez, Emily Days, Paige Newton Vinson, Krystian Andrezej Kozek, Charles David Weaver, Anna Louise Blobaum, Peter Jeffrey Conn, Colleen Marie Niswender, Craig William Lindsley | Challenges in the Discovery and Optimization of mGlu2/4 Heterodimer Positive Allosteric Modulators | Lett Drug Des Discov. 2019 Dec; 16(12): 1387-1394. |
Eileen Jackson, Marc Heidl, Dominik Imfeld, Laurent Meeus, Rolf Schuetz, Remo Campiche | Discovery of a Highly Selective MC1R Agonists Pentapeptide to Be Used as a Skin Pigmentation Enhancer and with Potential Anti-Aging Properties | Int J Mol Sci. 2019 Dec; 20(24): 6143. |
Hua Rong Lu, Haoyu Zeng, Ralf Kettenhofen, Liang Guo, Ivan Kopljar, Karel van Ammel, Fetene Tekle, Ard Teisman, Jin Zhai, Holly Clouse, Jennifer Pierson, Michael Furniss, Armando Lagrutta, Frederick Sannajust, David J Gallacher | Assessing Drug-Induced Long QT and Proarrhythmic Risk Using Human Stem-Cell-Derived Cardiomyocytes in a Ca2+ Imaging Assay: Evaluation of 28 CiPA Compounds at Three Test Sites | Toxicol Sci 2019 Aug 1;170(2):345-356. |
Ivan Kopljar, An N Hermans, Ard Teisman, David J Gallacher, Hua Rong Lu | Impact of calcium-sensitive dyes on the beating properties and pharmacological responses of human iPS-derived cardiomyocytes using the calcium transient assay | J Pharmacol Toxicol Methods . May-Jun 2018;91:80-86. |
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Tania Chernov-Rogan, Tianbo Li, Gang Lu, Henry Verschoof, Kuldip Khakh, Steven W. Jones, Maureen H. Beresini, Chang Liu, Daniel F. Ortwine, Steven J. McKerrall, David H. Hackos, Daniel Sutherlin, Charles J. Cohen, and Jun Chen | Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors | PNAS January 23, 2018 115 (4) E792-E801 |
Philippa Dale, Victoria Head, Mark R.Dowling, Colin W.Taylor | Selective inhibition of histamine-evoked Ca2+ signals by compartmentalized cAMP in human bronchial airway smooth muscle cells | Cell Calcium Volume 71, May 2018, Pages 53-64 |
Malika Faouzi, Ram P. Neupane, Jian Yang, Philip Williams & Reinhold Penner | Areca nut extracts mobilize calcium and release pro-infammatory cytokines from various immune cells | Scientific Reports 8, Article number: 1075 (2018) |
Stefan Just, Bertrand L. Chenard, Angelo Ceci, Timothy Strassmaier, Jayhong A. Chong , Nathaniel T. Blair, Randall J. Gallaschun , Donato del Camino, Susan Cantin, Marc D’Amours, Christian Eickmeier, Christopher M. Fanger, Carsten Hecker, David P. Hessler, Bastian Hengerer, Katja S. Kroker, Sam Malekiani, Robert Mihalek, Joseph McLaughlin, Georg Rast, JoAnn Witek, Achim Sauer,Christopher R. Pryce, Magdalene M. Moran | Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice | Published: January 31, 2018 https://doi.org/10.1371/journal.pone.0191225 |
Chun LS, Vekariya RH, Free RB, Li Y, Lin DT, Su P, Liu F, Namkung Y, Laporte SA, Moritz AE, Aube J, Frankowski KJ, Sibley DR. | Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor | Front Synaptic Neurosci. 2018; 10: 2. |
Kopljar I, Hermans AN, Teisman A, Gallacher DJ, Lu HR. | Impact of calcium-sensitive dyes on the beating properties and pharmacological responses of human iPS-derived cardiomyocytes using the calcium transient assay. | J Pharmacol Toxicol Methods. 2018 May - Jun;91:80-86. doi: 10.1016/j.vascn.2018.02.004. Epub 2018 Feb 6. |
Michael C. Burns, Jennifer E. Howes, Qi Sun, Andrew J. Little, DeMarco V. Camper, Jason R. Abbott, Jason Phan, Taekyu Lee, Alex G. Waterson, Olivia W. Rossanese, Stephen W. Fesik | High-throughput screening identifies small molecules that bind to the RAS: SOS: RAS complex and perturb RAS signaling | Anal Biochem. 2018 May 1; 548: 44-52. |
Suzuki S, Lis A, Schmitz C, Penner R, Fleig A | The TRPM7 kinase limits receptor-induced calcium release by regulating heterotrimeric G-proteins | Cell Mol Life Sci. 2018 Aug;75(16):3069-3078. doi: 10.1007/s00018-018-2786-z. Epub 2018 Mar 2. |
Stacey P, Wassermann AM, Kammonen L, Impey E, Wilbrey A, Cawkill D | Plate-Based Phenotypic Screening for Pain Using Human iPSC-Derived Sensory Neurons | SLAS Discov. 2018 Jul;23(6):585-596. doi: 10.1177/2472555218764678. Epub 2018 Mar 16. |
Aaron M. Bender, Hyekyung P. Cho, Kellie D. Nance, Kaelyn S. Lingenfelter, Vincent B. Luscombe, Patrick R. Gentry, Karl Voigtritter, Alice E. Berizzi, Patrick M. Sexton, Christopher J. Langmead , Arthur Christopoulos, Charles W. Locuson, Thomas M. Bridges, Sichen Chang, Jordan C. O’Neill, Xiaoyan Zhan, Colleen M. Niswender, Carrie K. Jones, P. Jeffrey Conn, and Craig W. Lindsley | Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold | ACS Chem Neurosci. 2018 Jul 18;9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126. Epub 2018 Apr 26. |
Jerri M. Rook, Jeanette L Bertron, Hyekyung P. Cho, Pedro M Garcia-Barrantes, Sean P Moran, James T Maksymetz, Kellie D Nance, Jonathan W Dickerson, Daniel H Remke, Sichen Chang, Joel Harp, Anna L. Blobaum, Colleen M Niswender, Carrie K. Jones, Shaun R. Stauffer, P. Jeffrey Conn, and Craig W Lindsley | A novel M1 PAM VU0486846 exerts efficacy in cognition models without displaying agonist activity or cholinergic toxicity | ACS Chem Neurosci. 2018 Sep 19;9(9):2274-2285. doi: 10.1021/acschemneuro.8b00131. Epub 2018 May 8. |
Tomoaki M. Kato, Mie Kubota-Sakashita, Noriko Fujimori-Tono, Fumihito Saito, Satoshi Fuke, Akira Masuda, Shigeyoshi Itohara, Hidenori Suzuki, Tadafumi Kato | Ant1 mutant mice bridge the mitochondrial and serotonergic dysfunctions in bipolar disorde | Molecular Psychiatry 23, 2039-2049 (2018) |
Yuki Kuramoto, Atsuhiko T.Naito Hiromas Tojo, Taku Sakai, Masamichi Ito, Masato Shibamoto, Akito Nakagawa, Tomoaki Higo, Katsuki Okada, Toshihiro Yamaguchi, Jong-Kook Lee, Shigeru Miyagawa, Yoshiki Sawa, Yasushi Sakata Issei Komuro | Generation of Fabry cardiomyopathy model for drug screening using induced pluripotent stem cell-derived cardiomyocytes from a female Fabry patient | Journal of Molecular and Cellular Cardiology Volume 121, August 2018, Pages 256-265 |
Luderman KD, Conroy JL, Free RB, Southall N, Ferrer M, Sanchez-Soto M, Moritz AE, Willette BKA, Fyfe TJ, Jain P, Titus S, Hazelwood LA, Aube J, Lane JR, Frankowski KJ, Sibley DR | Identification of Positive Allosteric Modulators of the D1 Dopamine Receptor That Act at Diverse Binding Sites | Mol Pharmacol. 2018 Oct; 94(4): 1197-1209. |
Agnieszka Krzyzosiak, Anna Sigurdardottir, Laura Luh, Marta Carrara, Indrajit Das, Kim Schneider, Anne Bertolotti | Target-Based Discovery of an Inhibitor of the Regulatory Phosphatase PPP1R15B | Cell. 2018 Aug 23; 174(5): 1216-1228.e19. |
Roy J.Vaza, Yi Lia, Vinolia Chellaraja, Stephan Reilinga, Theresa Kuntzweilera, Donglai Yang, Hong Shen, Joseph D.Batchelora, Ying Zhang, Xin Chen, Larry R.McLean, Raymond Kosley Jr. | Amelioration of PXR-mediated CYP3A4 induction by mGluR2 modulators | Bioorg Med Chem Lett. 2018 Oct 15;28(19):3194-3196. doi: 10.1016/j.bmcl.2018.08.022. Epub 2018 Aug 20. |
Takahiro Yamazaki, Yumie Morimoto-Kobayashi, Kumiko Koizumi, Chika Takahashi, Shiori Nakajima, Sayoko Kitao, Yoshimasa Taniguchi, Mikio Katayama, Yoshihiro Ogawa | Secretion of a gastrointestinal hormone, cholecystokinin, by hop-derived bitter components activates sympathetic nerves in brown adipose tissue | The Journal of Nutritional Biochemistry Volume 64, February 2019, Pages 80-87 |
Anton L. Martinez, Jose Brea, Xavier Monroy, Manuel Merlos, Javier Burgueno, Maria Isabel Loza | A New Model of Sensorial Neuron-Like Cells for HTS of Novel Analgesics for Neuropathic Pain | SLAS Discov. 2019 Feb;24(2):158-168. doi: 10.1177/2472555218810323. Epub 2018 Nov 1. |
Hirotaka Mizuno, Yasuyuki Kihara, Amanda Kussrow, Allison Chen, Manisha Ray, Richard Rivera, Darryl J. Bornhop, and Jerold Chun | Lysophospholipid G protein-coupled receptor binding parameters as determined by backscattering interferometry | J Lipid Res. 2019 Jan;60(1):212-217. doi: 10.1194/jlr.D089938. Epub 2018 Nov 21. |
Ivan Kopljar, Hua Rong Lu, Karel Van Ammel, Martin Otava, Fetene Tekle, Ard Teisman, David J.Gallacher | Development of a Human iPSC Cardiomyocyte-Based Scoring System for Cardiac Hazard Identification in Early Drug Safety De-risking | Stem Cell Reports. 2018 Dec 11; 11(6): 1365-1377. |
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Yasuhiro Wada, Hiromitsu Shirahashi, Taisuke Iwanami, Masami Ogawa, Seiji Nakano, Akifumi Morimoto, Ken-ichi Kasahara, Eiichi Tanaka, Yoshio Takada, Shigeki Ohashi, Mutsuhiro Mori, Satoshi Shuto | Discovery of Novel Indazole Derivatives as Highly Potent and Selective Human β3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects | J Med Chem. 2015 Aug 13;58(15):6048-57. doi: 10.1021/acs.jmedchem.5b00638. Epub 2015 Jul 15. |
Icilio Cavero, Henry Holzgrefe | CiPA: Ongoing testing, future qualification procedures, and pending issues | J Pharmacol Toxicol Methods. 2015 Nov-Dec;76:27-37. doi: 10.1016/j.vascn.2015.06.004. Epub 2015 Jul 6. |
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Cheryl de Valliere, Solange Vidal, Ieuan Clay, Giorgia Jurisic, Irina Tcymbarevich, Silvia Lang, Marie-Gabrielle Ludwig, Michal Okoniewski, Jyrki J. Eloranta, Gerd A. Kullak-Ublick, Carsten A. Wagner, Gerhard Rogler, Klaus Seuwen | The pH-sensing receptor OGR1 improves barrier function of epithelial cells and inhibits migration in an acidic environment | Am J Physiol Gastrointest Liver Physiol. 2015 Sep 15;309(6):G475-90. doi: 10.1152/ajpgi.00408.2014. Epub 2015 Jul 23. |
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Emi Shoji, Hidetoshi Sakurai, Tokiko Nishino, Tatsutoshi Nakahata, Toshio Heike, Tomonari Awaya, Nobuharu Fujii, Yasuko Manabe, Masafumi Matsuo, Atsuko Sehara-Fujisawa | Early pathogenesis of Duchenne muscular dystrophy modelled in patient-derived human induced pluripotent stem cells | Sci Rep. 2015 Aug 20;5:12831. doi: 10.1038/srep12831. |
Yasuo Yonetomi, Tomohiko Sekioka, Michiaki Kadode, Tetsuya Kitamine, Akihiro Kamiya, Atsuto inoue, Takafumi Nakao, Hiroaki Nomura, Masayuki Murata, Shintaro Nakao, Fumio Nambu, Manabu Fujita, Shinji Nakade, Kazuhito Kawabata | Effects of ONO-6950, a novel dual cysteinyl leukotriene 1 and 2 receptors antagonist, in a guinea pig model of asthma | Eur J Pharmacol. 2015 Oct 15;765:242-8. doi: 10.1016/j.ejphar.2015.08.041. Epub 2015 Aug 28. |
Atsushi Nakane, Yusuke Gotoh, Junji Ichihara, Hidetaka Nagata | New screening strategy and analysis for identification of allosteric modulators for glucagon-like peptide-1 receptor using GLP-1 (9-36) amide | Anal. Biochem. 2015 Dec 15;491:23-30. doi: 10.1016/j.ab.2015.08.026. Epub 2015 Sep 2. |
Jae Wan Jang, Nam-Chul Cho, Sun-Joon Min, Yong Seo Cho, Ki Duk Park, Seon Hee Seo, Kyoung Tai No, Ae Nim Pae | Novel Scaffold Identification of mGlu1 Receptor Negative Allosteric Modulators Using a Hierarchical Virtual Screening Approach | Chem Biol Drug Des. 2016 Feb;87(2):239-56. doi: 10.1111/cbdd.12654. Epub 2015 Oct 9. |
Yoshiharu Uruno, Yasuko Konishi, Atsushi Suwa, Kentaro Takai, Kengo Tojo, Tomokazu Nakako, Mutsuko Sakai, Takeshi Enomoto, Harumi Matsuda, Atsushi Kitamura, Takaaki Sumiyoshi | Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M1 and M4 muscarinic acetylcholine receptors agonists | Bioorg Med Chem Lett. 2015 Nov 15;25(22):5357-61. doi: 10.1016/j.bmcl.2015.09.032. Epub 2015 Sep 12. |
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Brian Tomkowicz, Eileen Walsh, Adam Cotty, Raluca Verona, Nina Sabins, Fred Kaplan, Sandy Santulli-Marotto, Chen-Ni Chin, Jill Mooney, Russell B. Lingham, Michael Naso, Timothy McCabe | TIM-3 Suppresses Anti-CD3/CD28-Induced TCR Activation and IL-2 Expression through the NFAT Signaling Pathway | PLoS One. 2015 Oct 22;10(10):e0140694. doi: 10.1371/journal.pone.0140694. eCollection 2015. |
Hilary Highfield Nickols, Joannes P. Yuh, Karen J. Gregory, Ryan D. Morrison, Brittney S. Bates, Shaun R. Stauffer, Kyle A. Emmitte, Michael Bubser, Weimin Peng, Michael T. Nedelcovych, Analisa Thompson, Xiaohui Lv, Zixiu Xiang, J. Scott Daniels, Colleen M. Niswender, Craig W. Lindsley, Carrie K. Jones,P. Jeffrey Conn | VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy | J Pharmacol Exp Ther. 2016 Jan;356(1):123-36. doi: 10.1124/jpet.115.226597. Epub 2015 Oct 26. |
Jesse A. May, Najam A. Sharif, Marsha A. McLaughlin, Hwang-Hsing Chen, Bryon S. Severns, Curtis R. Kelly, William F. Holt, Richard Young, Richard A. Glennon, Mark R. Hellberg, Thomas R. Dean | Ocular Hypotensive Response in Nonhuman Primates of (8R)-1-[(2S)-2-Aminopropyl]-8,9-dihydro-7H-pyrano[2,3-g]indazol-8-ol a Selective 5-HT2 Receptor Agonist | J Med Chem. 2015 Nov 25;58(22):8818-33. doi: 10.1021/acs.jmedchem.5b00857. Epub 2015 Nov 9. |
Hoang Nam Vu, Ji Young Kim, Ahmed H.E. Hassan, Kihang Choi Jong-Hyun Park, Ki Duk Park, Jae Kyun Lee, Ae Nim Pae, Hyunah Choo, Sun-Joon Min, Yong Seo Cho | Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists | Bioorg Med Chem Lett. 2016 Jan 1;26(1):140-4. doi: 10.1016/j.bmcl.2015.11.012. Epub 2015 Nov 5. |
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Hiroyuki Koyama, Hiroshi Iwakura, Katsuko Dote, Mika Bando, Hiroshi Hosoda, Hiroyuki Ariyasu, Toru Kusakabe, Choel Son, Kiminori Hosoda, Takashi Akamizu, Kenji Kangawa, Kazuwa Nakao | Comprehensive Profiling of GPCR Expression in Ghrelin-producing Cells | Endocrinology. 2016 Feb;157(2):692-704. doi: 10.1210/en.2015-1784. Epub 2015 Dec 15. |
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Authors | Title | Source |
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Anke Bill, Elizabeth M. Rosethorne, Toby C. Kent, Lindsay Fawcett, Lynn Burchell, Michiel T. van Diepen, Anthony Marelli, Sergey Batalov, Loren Miraglia, Anthony P. Orth, Nicole A. Renaud, Steven J. Charlton, Martin Gosling, L. Alex Gaither, Paul J. Groot-Kormelink | High Throughput Mutagenesis for Identification of Residues Regulating Human Prostacyclin (hIP) Receptor Expression and Function | PLoS One. 2014 Jun 2;9(6):e97973. doi: 10.1371/journal.pone.0097973. eCollection 2014. |
Anke Bill, M. Oana Popa, Michiel T. van Diepen, Abraham Gutierrez, Sarah Lilley, Maria Velkova, Kathryn Acheson, Hedaythul Choudhury, Nicole A. Renaud, Douglas S. Auld, Martin Gosling, Paul J. Groot-Kormelink, L. Alex Gaither | Variomics Screen Identifies the Re-entrant Loop of the Calcium-activated Chloride Channel ANO1 That Facilitates Channel Activation | J Biol Chem. 2015 Jan 9;290(2):889-903. doi: 10.1074/jbc.M114.618140. Epub 2014 Nov 25. |
Ann-Beth Norholm, Pierre Francotte, Eric Goffin, Iuliana Botez, Laurence Danober, Pierre Lestage, Bernard Pirotte, Jette S. Kastrup, Lars Olsen, Chris Oostenbrink | Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces | J Chem Inf Model. 2014 Dec 22;54(12):3404-16. doi: 10.1021/ci500559b. Epub 2014 Dec 9. |
Anuradha Roy | High Throughput Screening Operations at the University of Kansas | Comb Chem High Throughput Screen. 2014 May;17(4):387-93. |
Bin Cai, Xia Chen, Fang Liu, Jun Li, Lijuan Gu, Jason R. Liu, Jay Liu | A Cell-Based Functional Assay Using a Green Fluorescent Protein-Based Calcium Indicator dCys-GCaMP | Assay Drug Dev Technol. 2014 Aug;12(6):342-51. doi: 10.1089/adt.2014.584. Epub 2014 Aug 8. |
Cheryse A. Furman, Rebecca A. Roof, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, R. Benjamin Free, Ashwini K. Banala, Noel M. Paul, Vivek Kumar, Christopher D. Sibley, Amy Hauck Newman, David R. Sibley | Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists | Eur Neuropsychopharmacol. 2014 Nov 29. pii: S0924-977X(14)00324-1. doi: 10.1016/j.euroneuro.2014.11.013. [Epub ahead of print] |
Eunan Hendron, Xizhuo Wang, Yandong Zhou, Xiangyu Cai, Jun-Ichi Goto, Katsuhiko Mikoshiba, Yoshihiro Baba, Tomohiro Kurosaki, Youjun Wang, Donald L. Gill | Potent functional uncoupling between STIM1 and Orai1 by dimeric 2-aminodiphenyl borinate analogs | Cell Calcium. 2014 Oct 23;56(6):482-492. doi: 10.1016/j.ceca.2014.10.005. [Epub ahead of print] |
Frederic Bassilana, Adam Carlson, Jennifer A DaSilva, Bianka Grosshans, Solange Vidal, Valerie Beck, Barbara Wilmeringwetter, Luis A Llamas, Todd B Showalter, Pascal Rigollier, Aaron Bourret, Arun Ramamurthy, Xu Wu, Fred Harbinski, Samantha Plonsky, Lac Lee, Heinz Ruffner, Paola Grandi, Markus Schirle, Jeremy Jenkins, Andreas W Sailer, Tewis Bouwmeester, Jeffrey A Porter, Vic Myer, Peter M Finan et al. | Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39 | Nat Chem Biol. 2014 May;10(5):343-9. doi: 10.1038/nchembio.1481. Epub 2014 Mar 16. |
Hongkang Zhang, Beiyan Zou, Fang Du, Kaiping Xu, and Min Li | Reporting Sodium Channel Activity Using Calcium Flux: Pharmacological Promiscuity of Cardiac Nav1.5 | Mol Pharmacol. 2015 Feb;87(2):207-17. doi: 10.1124/mol.114.094789. Epub 2014 Nov 24. |
Hyekyung P. Cho, Darren W. Engers, Daryl F. Venable, Colleen M. Niswender, Craig W. Lindsley, P. Jeffrey Conn, Kyle A. Emmitte, Alice L. Rodriguez | A Novel Class of Succinimide-Derived Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Provides Insight into a Disconnect in Activity between the Rat and Human Receptors | ACS Chem Neurosci. 2014 Jul 16;5(7):597-610. doi: 10.1021/cn5000343. Epub 2014 May 15. |
Hyekyung P. Cho, Pedro M. Garcia-Barrantes, John T. Brogan, Corey R. Hopkins, Colleen M. Niswender, Alice L. Rodriguez, Daryl F. Venable, Ryan D. Morrison, Michael Bubser, J. Scott Daniels, Carrie K. Jones, P. Jeffrey Conn, Craig W. Lindsley | Chemical Modulation of Mutant mGlu1 Receptors Derived from Deleterious GRM1 Mutations Found in Schizophrenics | ACS Chem Biol. 2014 Oct 17;9(10):2334-46. doi: 10.1021/cb500560h. Epub 2014 Aug 28. |
J. Kyle Bruner, Beiyan Zou, Hongkang Zhang, Yixin Zhang, Katharina Schmidt, Min Li | Identification of novel small molecule modulators of K2P18.1 two-pore potassium channel | Eur J Pharmacol. 2014 Oct 5;740:603-10. doi: 10.1016/j.ejphar.2014.06.021. Epub 2014 Jun 24. |
Jesse E. Hanson, William J. Meilandt, Alvin Gogineni, Paul Reynen, James Herrington, Robby M. Weimer, Kimberly Scearce-Levie, Qiang Zhou | Chronic GluN2B Antagonism Disrupts Behavior in Wild-Type Mice Without Protecting Against Synapse Loss or Memory Impairment in Alzheimer's Disease Mouse Models | J Neurosci. 2014 Jun 11;34(24):8277-88. doi: 10.1523/JNEUROSCI.5106-13.2014. |
John W. Kehoe, Brian Whitaker, Deidra Bethea, Eilyn R. Lacy, Ken Boakye, Sandra Santulli-Marotto, Mary H. Ryan, Yiqing Feng, John C. WheelerJohn W. Kehoe, Brian Whitaker, Deidra Bethea, Eilyn R. Lacy, Ken Boakye, Sandra Santulli-Marotto, Mary H. Ryan, Yiqing Feng, John C. Wheeler | Isolation and optimization for affinity and biophysical characteristics of anti-CCL17 antibodies from the VH1-69 germline gene | Protein Eng Des Sel. 2014 Jun;27(6):199-206. doi: 10.1093/protein/gzu012. Epub 2014 Apr 16. |
Julie A. Meade, R. Benjamin Free, Nicole R. Miller, Lani S. Chun, Trevor B. Doyle, Amy E. Moritz, Jennie L. Conroy, Val J. Watts, David R. Sibley | (-)-Stepholidine is a potent pan-dopamine receptor antagonist of both G protein- and β-arrestin-mediated signaling | Psychopharmacology (Berl). 2014 Sep 18. [Epub ahead of print] |
Junki Miyamoto, Taichi Mizukure, Si-Bum Park, Shigenobu Kishino, Ikuo Kimura, Kanako Hirano, Paolo Bergamo, Mauro Rossi, Takuya Suzuki, Makoto Arita, Jun Ogawa, Soichi Tanabe | A gut microbial metabolite of linoleic acid, 10-hydroxy-cis-12-octadecenoic acid, ameliorates intestinal epithelial barrier impairment partially via GPR40/MEK-ERK pathway | J Biol Chem. 2014 Dec 10. pii: jbc.M114.610733. [Epub ahead of print] |
Kazuyuki Fukushima, Yoshikuni Tabata, Yoichi Imaizumi, Naohiro Kohmura, Michiko Sugawara, Kohei Sawada, Kazuto Yamazaki, Masashi Ito | Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to Physiologically Relevant Assays for Multiple Ionotropic Glutamate Receptors | J Biomol Screen. 2014 Jun 30;19(8):1174-1184. [Epub ahead of print] |
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Lindsey C. Morris, Emily L. Days, Maxine Turney, Dehui Mi, Craig W. Lindsley, C. David Weaver, Kevin D. Niswender | A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors | J Biomol Screen. 2014 Feb 13;19(6):847-858. [Epub ahead of print] |
Matthew F. Rouhier, Rene Raphemot, Jerod S. Denton, Peter M. Piermarini | Pharmacological Validation of an Inward-Rectifier Potassium (Kir) Channel as an Insecticide Target in the Yellow Fever MosquitoAedes aegypti | PLoS One. 2014 Jun 24;9(6):e100700. doi: 10.1371/journal.pone.0100700. eCollection 2014. |
Michael P. Winters, Nalin Subasinghe, Mark Wall, Edward Beck, Michael R. Brandt, Michael F.A. Finley, Yi Liu, Mary Lou Lubin, Michael P. Neeper, Ning Qin, Christopher M. Flores, Zhihua Sui | Discovery and SAR of novel tetrahydropyrrolo[3,4-c]pyrazoles as inhibitors of the N-type calcium channel | Bioorg Med Chem Lett. 2014 May 1;24(9):2053-6. doi: 10.1016/j.bmcl.2014.03.062. Epub 2014 Mar 27. |
Mikkel A. Rasmussen, Bjorn Holst, Zeynep Tumer, Mads G. Johnsen, Shuling Zhou, Tina C. Stummann, Poul Hyttel, Christian Clausen | Transient p53 Suppression Increases Reprogramming of Human Fibroblasts without Affecting Apoptosis and DNA Damage | Stem Cell Reports. 2014 Sep 9;3(3):404-13. doi: 10.1016/j.stemcr.2014.07.006. Epub 2014 Aug 21. |
Mingfei Ji, Xubo Su, Xiaohong Su, Yingyi Chen, Wenkang Huang, Jian Zhang, Zhaobin Gao, Chuangang Li, Xuefeng Lu | Identification of Novel Compounds for Human Bitter Taste Receptors | Chem Biol Drug Des. 2014 Jul;84(1):63-74. doi: 10.1111/cbdd.12293. Epub 2014 Feb 28. |
Nidhi Jalan-Sakrikar, Julie R. Field, Rebecca Klar, Margrith E. Mattmann, Karen J. Gregory, Rocio Zamorano, Darren W. Engers, Sean R. Bollinger, C. David Weaver, Emily L. Days, L. Michelle Lewis, Thomas J. Utley, Miguel Hurtado, Delphine Rigault, Francine Acher, Adam G. Walker, Bruce J. Melancon, Michael R. Wood, Craig W. Lindsley, P. Jeffrey Conn, Zixiu Xiang, Corey R. Hopkins, and Colleen M. Niswender | Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7 | ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37. doi: 10.1021/cn500153z. Epub 2014 Oct 9. |
R. Benjamin Free, Lani S. Chun, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, Jennie L. Conroy, Adrian Padron, Julie A. Meade, Jingbo Xiao, Xin Hu, Andres E. Dulcey, Yang Han, Lihua Duan, Steve Titus, Melanie Bryant-Genevier, Elena Barnaeva, Marc Ferrer, Jonathan A. Javitch, Thijs Beuming, Lei Shi, Noel T. Southall, Juan J. Marugan, David R. Sibley | Discovery and Characterization of a G Protein—Biased Agonist That Inhibits β-Arrestin Recruitment to the D2 Dopamine Receptor | Mol Pharmacol. 2014 Jul;86(1):96-105. doi: 10.1124/mol.113.090563. Epub 2014 Apr 22. |
Rene Raphemot, Matthew F. Rouhier, Daniel R. Swale, Emily Days, C. David Weaver, Kimberly M. Lovell, Leah C. Konkel, Darren W. Engers, Sean F. Bollinger, Corey Hopkins, Peter M. Piermarini , Jerod S. Denton | Discovery and Characterization of a Potent and Selective Inhibitor of Aedes aegypti Inward Rectifier Potassium Channels | PLoS One. 2014 Nov 6;9(11):e110772. doi: 10.1371/journal.pone.0110772. eCollection 2014. |
Wendy J. Winchester, Katrina Gore, Sophie Glatt, Wendy Petit, Jennifer C. Gardiner, Kelly Conlon, Michael Postlethwaite, Pierre-Philippe Saintot, Sonia Roberts, James R. Gosset, Tomomi Matsuura, Mark D. Andrews, Paul A. Glossop, Michael J. Palmer, Nicola Clear, Susie Collins, Kevin Beaumont, David S. Reynolds | Inhibition of TRPM8 Channels Reduces Pain in the Cold Pressor Test in Humans | J Pharmacol Exp Ther. 2014 Nov;351(2):259-69. doi: 10.1124/jpet.114.216010. Epub 2014 Aug 14. |
Zhiqiang Wang, Shimeng Liu, Miyo Kakizaki, Yuuki Hirose, Yukiko Ishikawa, Hiromasa Funato, Masashi Yanagisawa, Yonghao Yu, Qinghua Liu | Orexin/Hypocretin Activates mTOR Complex 1 (mTORC1) via an Erk/Akt-independent and Calcium-stimulated Lysosome v-ATPase Pathway | J Biol Chem. 2014 Nov 14;289(46):31950-9. doi: 10.1074/jbc.M114.600015. Epub 2014 Oct 2. |
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Andrew J. Storaska, Jian P. Mei, Meng Wu, Min Li, Susan M. Wade, Levi L. Blazer, Benita Sjogren, Corey R. Hopkins, Craig W. Lindsley, Zhihong Lin, Joseph J. Babcock, Owen McManus, Richard R. Neubig | Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay | Cell Signal. 2013 Dec;25(12):2848-55. doi: 10.1016/j.cellsig.2013.09.007. Epub 2013 Sep 14. |
C Brenneis, K Kistner, M Puopolo, S Jo, DP Roberson, M Sisignano, D Segal, E J Cobos, B J Wainger, S Labocha, N Ferreiros, C von Hehn, J Tran, G Geisslinger, P W Reeh, B P Bean, C J Woolf | Bupivacaine-induced cellular entry of QX-314 and its contribution to differential nerve block | Br J Pharmacol. 2014 Jan;171(2):438-51. doi: 10.1111/bph.12466. |
Erica VanderPorten, Lauren Frick, Rebecca Turincio, Peter Thana, William LaMarr, Yichin Liu | Label-free high-throughput assays to screen and characterize novel lactate dehydrogenase inhibitors | Anal Biochem. 2013 Oct 15;441(2):115-22. doi: 10.1016/j.ab.2013.07.003. Epub 2013 Jul 16. |
Florian P. M. Kohn | High Throughput Fluorescent Screening of Membrane Potential and Intracellular Calcium Concentration Under Variable Gravity Conditions | Microgravity Sci. Technol. 2013 April, Volume 25, Issue 2, pp 113-120. doi: 10.1007/s12217-012-9331-8 |
Hilde Lavreysen, Xavier Langlois, Abdel Ahnaou, Wilhelmus Drinkenburg, Paula te Riele, Ilse Biesmans, Ilse Van der Linden, Luc Peeters, Anton Megens, Cindy Wintmolders, Jose Maria Cid, Andres A. Trabanco, Jose Ignacio Andres, Frank M. Dautzenberg, Robert Lutjens, Gregor Macdonald, John R. Atack | Pharmacological Characterization of JNJ-40068782, a New Potent, Selective, and Systemically Active Positive Allosteric Modulator of the mGlu2 Receptor and Its Radioligand [3H]JNJ-40068782 | J Pharmacol Exp Ther. 2013 Sep;346(3):514-27. doi: 10.1124/jpet.113.204990. Epub 2013 Jun 13. |
Jason T. Manka, Alice L. Rodriguez, Ryan D. Morrison, Daryl F. Venable, Hyekyung P. Cho, Anna L. Blobaum, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte | Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1 | Bioorg Med Chem Lett. 2013 Sep 15;23(18):5091-6. doi: 10.1016/j.bmcl.2013.07.029. Epub 2013 Jul 23. |
Kentaro Ozawa, Akira T. Komatsubara, Yuhei Nishimura, Tomoyo Sawada, Hiroto Kawafune, Hiroki Tsumoto, Yuichi Tsuji, Jing Zhao, Yoji Kyotani, Toshio Tanaka, Ryosuke Takahashi, Masanori Yoshizumi | S-nitrosylation regulates mitochondrial quality control via activation of parkin | Sci Rep. 2013;3:2202. doi: 10.1038/srep02202. |
Kentaro Takai, Yasunao Inoue, Yasuko Konishi, Atsushi Suwa, Yoshiharu Uruno, Harumi Matsuda, Tomokazu Nakako, Mutsuko Sakai, Hiroyuki Nishikawa, Gakuji Hashimoto, Takeshi Enomoto, Atsushi Kitamura, Yasuaki Uematsu, Akihiko Kiyoshi, Takaaki Sumiyoshi | Identification of N-substituted 8-azatetrahydroquinolone derivatives as selective and orally active M1 and M4 muscarinic acetylcholine receptors agonists | Bioorg Med Chem Lett. 2013 Aug 15;23(16):4644-7. doi: 10.1016/j.bmcl.2013.06.013. Epub 2013 Jun 13. |
Kimberly M. Lovell, Andrew S. Felts, Alice L. Rodriguez, Daryl F. Venable, Hyekyung P. Cho, Ryan D. Morrison, Frank W. Byers, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte | N-Acyl-N′-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats | Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. doi: 10.1016/j.bmcl.2013.05.020. Epub 2013 May 17. |
Lani S. Chun, R. Benjamin Free, Trevor B. Doyle, Xi-Ping Huang, Michele L. Rankin, David R. Sibley | D1-D2 Dopamine Receptor Synergy Promotes Calcium Signaling via Multiple Mechanisms | Mol Pharmacol. 2013 Aug;84(2):190-200. doi: 10.1124/mol.113.085175. Epub 2013 May 16. |
Mamoru Tasakia, Miki Kobayashi, Yoshiyuki Tenda, Susumu Tsujimoto, Shoko Nakazato, Mako Numazaki, Yasuno Hirano, Hiroshi Matsuda, Tadashi Terasaka, Yasuhiro Miyao, Yasuaki Shimizu, Yoshitaka Hirayama | Inhibition of antigen-induced airway inflammation and hyperresponsiveness in guinea pigs by a selective antagonist of “chemoattractant receptor homologous molecule expressed on Th2 cells” (CRTH2) | Eur J Pharm Sci. 2013 Jun 14;49(3):434-40. doi: 10.1016/j.ejps.2013.04.017. Epub 2013 Apr 24. |
Paul H. Tewson, Anne Marie Quinn, Thomas E. Hughes | A Multiplexed Fluorescent Assay for Independent Second-Messenger Systems Decoding GPCR Activation in Living Cells |
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Rene Raphemot, C. David Weaver, Jerod S. Denton | High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels | J Vis Exp. 2013 Jan 27;(71). pii: 4209. doi: 10.3791/4209. |
Rene Raphemot, Matthew F. Rouhier, Rocco D. Gogliotti, Kimberly M. Lovell, Rebecca M. Hine, Dhairyasheel Ghosalkar, Anthony Longo, Klaus W. Beyenbach, Jerod S. Denton, Peter M. Piermarini | Eliciting Renal Failure in Mosquitoes with a Small-Molecule Inhibitor of Inward-Rectifying Potassium Channels | PLoS One. 2013 May 29;8(5):e64905. doi: 10.1371/journal.pone.0064905. Print 2013. |
Samarjit Patnaik, Juan J. Marugan, Ke Liu, Wei Zheng, Noel Southall, Seameen J. Dehdashti, Annika Thorsell, Markus Heilig, Lauren Bell, Michelle Zook, Bob Eskay, Kyle R. Brimacombe, Christopher P. Austin | Structure—Activity Relationship of Imidazopyridinium Analogues as Antagonists of Neuropeptide S Receptor | J Med Chem. 2013 Nov 27;56(22):9045-56. doi: 10.1021/jm400904m. Epub 2013 Nov 11. |
Sandra Santulli-Marotto, Jamie Fisher, Theodore Petley, Ken Boakye, Tadas Panavas, Jennifer Luongo, Karl Kavalkovich, Michael Rycyzyn, Bingyuan Wu, Lester Gutshall, Ana Coelho, Cory M. Hogaboam, Mary Ryan | Surrogate Antibodies That Specifically Bind and Neutralize CCL17 But Not CCL22 | Monoclon Antib Immunodiagn Immunother. 2013 Jun;32(3):162-71. doi: 10.1089/mab.2012.0112. |
Sandra Santulli-Marotto, Ken Boakye, Eilyn Lacy, Sheng-Jiun Wu, Jennifer Luongo, Karl Kavalkovich, Ana Coelho, Cory M. Hogaboam, Mary Ryan | Engagement of Two Distinct Binding Domains on CCL17 Is Required for Signaling through CCR4 and Establishment of Localized Inflammatory Conditions in the Lung | PLoS One. 2013 Dec 5;8(12):e81465. doi: 10.1371/journal.pone.0081465. eCollection 2013. |
Sebastien Hannedouche, Valerie Beck, Juliet Leighton-Davies, Martin Beibel, Guglielmo Roma, Edward J. Oakeley, Vincent Lannoy, Jerome Bernard, Jacques Hamon, Samuel Barbieri, Inga Preuss, Marie-Christine Lasbennes, Andreas W. Sailer, Thomas Suply, Klaus Seuwen, Christian N. Parker, Frederic Bassilana | Identification of the C3a Receptor (C3AR1) as the Target of the VGF-derived Peptide TLQP-21 in Rodent Cells | J Biol Chem. 2013 Sep 20;288(38):27434-43. doi: 10.1074/jbc.M113.497214. Epub 2013 Aug 12. |
Shoichiro Ozaki, Akinobu Z. Suzuki, Peter O. Bauer, Etsuko Ebisui, Katsuhiko Mikoshiba | 2-Aminoethyl diphenylborinate (2-APB) analogues: Regulation of Ca2+ signaling | Biochem Biophys Res Commun. 2013 Nov 15;441(2):286-90. doi: 10.1016/j.bbrc.2013.08.102. Epub 2013 Sep 11. |
Summer E. Young, Matthew T. Duvernay, Michael L. Schulte, Craig W. Lindsley, Heidi E. Hamm | Synthesis of Indole Derived Protease-Activated Receptor 4 Antagonists and Characterization in Human Platelets | PLoS One. 2013 Jun 11;8(6):e65528. doi: 10.1371/journal.pone.0065528. Print 2013. |
Susan J. Ramos-Hunter, Darren W. Engers, Kristian Kaufmann, Yu Du, Craig W. Lindsley, C. David Weaver, Gary A. Sulikowski | Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators | Bioorg Med Chem Lett. 2013 Sep 15;23(18):5195-8. doi: 10.1016/j.bmcl.2013.07.002. Epub 2013 Jul 18. |
Thomas M. Bridges, Jerri M. Rook, Meredith J. Noetzel, Ryan D. Morrison, Ya Zhou, Rocco D. Gogliotti, Paige N. Vinson, Zixiu Xiang, Carrie K. Jones, Colleen M. Niswender, Craig W. Lindsley, Shaun R. Stauffer, P. Jeffrey Conn, J. Scott Daniels | Biotransformation of a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Contributes to Seizure-Like Adverse Events in Rats Involving a Receptor Agonism-Dependent Mechanism | Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2. |
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Bo-Hye Im, Hyewhon Rhim | GABAB receptor-mediated ERK1/2 phosphorylation via a direct interaction with CaV1.3 channels | Neurosci Lett. 2012 Mar 28;513(1):89-94. doi: 10.1016/j.neulet.2012.02.014. Epub 2012 Feb 14. |
Caroline Chambon, Claudia Jatzke, Nico Wegener, Andreas Gravius, Wojciech Danysz | Using cholinergic M1 receptor positive allosteric modulators to improve memory via enhancement of brain cholinergic communication | Eur J Pharmacol. 2012 Dec 15;697(1-3):73-80. doi: 10.1016/j.ejphar.2012.10.011. Epub 2012 Oct 17. |
Christina Molck, Kasper Harpsoe, David E. Gloriam, Rasmus P. Clausen, Ulf Madsen, Lars O. Pedersen, Hermogenes N. Jimenez, Soren M. Nielsen, Jesper M. Mathiesen, Hans Brauner-Osborne | Pharmacological Characterization and Modeling of the Binding Sites of Novel 1,3-Bis(pyridinylethynyl)benzenes as Metabotropic Glutamate Receptor 5-Selective Negative Allosteric Modulators | Mol Pharmacol. 2012 Nov;82(5):929-37. doi: 10.1124/mol.112.078808. Epub 2012 Aug 16. |
DAVID C. RINKER, PATRICK L. JONES, R. JASON PITTS, MICHAEL RUTZLER, GRAY CAMP, LUJUAN SUN, PINGXI XU, DANIEL C. DORSET, DAVID WEAVER, LAURENCE J. ZWIEBEL | Novel high-throughput screens of Anopheles gambiae odorant receptors reveal candidate behaviour-modifying chemicals for mosquitoes | Physiol Entomol. 2012;37:33-41 doi: 10.1111/j.1365-3032.2011.00821.x |
Dinesh Puppala, Leon P. Collis, Sunny Z. Sun, Vinicius Bonato, Xian Chen, Blake Anson, Mathew Pletcher, Bernard Fermini, Sandra J. Engle | Comparative Gene Expression Profiling in Human-Induced Pluripotent Stem Cell—Derived Cardiocytes and Human and Cynomolgus Heart Tissue | Toxicol Sci. 2013 Jan;131(1):292-301. doi: 10.1093/toxsci/kfs282. Epub 2012 Sep 14. |
Franck Potet, Amanda N. Lorinc, Sebastien Chaigne, Corey R. Hopkins, Raghav Venkataraman, Svetlana Z. Stepanovic, L. Michelle Lewis, Emily Days, Veniamin Y. Sidorov, Darren W. Engers, Beiyan Zou, David Afshartous, Alfred L. George Jr., Courtney M. Campbell, Jeffrey R. Balser, Min Li, Franz J. Baudenbacher, Craig W. Lindsley, C. David Weaver, Sabina Kupershmidt | Identification and Characterization of a Compound That Protects Cardiac Tissue from Human Ether-a-go-go-related Gene (hERG)-related Drug-induced Arrhythmias | J Biol Chem. 2012 Nov 16;287(47):39613-25. doi: 10.1074/jbc.M112.380162. Epub 2012 Oct 2. |
Heinz Ruffner, Joelle Sprunger, Olga Charlat, Juliet Leighton-Davies, Bianka Grosshans, Adrian Salathe, Svenja Zietzling, Valerie Beck, Maxime Therier, Andrea Isken, Yang Xie, Yue Zhang, Huaixiang Hao, Xiaoying Shi, Dong Liu, Qinhui Song, Ieuan Clay, Gabriele Hintzen, Jan Tchorz, Laure C. Bouchez, Gregory Michaud, Peter Finan, Vic E. Myer, Tewis Bouwmeester, Jeff Porter, Marc Hild, Fred Bassilana, Christian N. Parker, Feng Cong | R-Spondin Potentiates Wnt/β-Catenin Signaling through Orphan Receptors LGR4 and LGR5 | PLoS One. 2012;7(7):e40976. doi: 10.1371/journal.pone.0040976. Epub 2012 Jul 16. |
India C. Severin, Adriano L.S. Souza, Jonathan H. Davis, Najia Musolino, Matthias Mack, Christine A. Power, Amanda E.I. Proudfoot | Properties of 7ND—CCL2 are modulated upon fusion to Fc | Protein Eng Des Sel. 2012 May;25(5):213-22. doi: 10.1093/protein/gzs008. Epub 2012 Mar 2. |
Jack Bergman, Rebecca A. Roof, Cheryse A. Furman, Jennie L. Conroy, Nancy K. Mello, David R. Sibley, Phil Skolnick | Modification of cocaine self-administration by buspirone (busparR): potential involvement of D3 and D4 dopamine receptors | Int J Neuropsychopharmacol. 2013 Mar;16(2):445-58. doi: 10.1017/S1461145712000661. Epub 2012 Jul 25. |
James M. Salovich, Paige N. Vinson, Douglas J. Sheffler, Atin Lamsal, Thomas J. Utley, Anna L. Blobaum, Thomas M. Bridges, Uyen Le, Carrie K. Jones, Michael R. Wood, J. Scott Daniels, P. Jeffrey Conn, Colleen M. Niswender, Craig W. Lindsley, Corey R. Hopkins | Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor | Bioorg Med Chem Lett. 2012 Aug 1;22(15):5084-8. doi: 10.1016/j.bmcl.2012.05.109. Epub 2012 Jun 6. |
Jingbo Xiao, R. Benjamin Free, Elena Barnaeva, Jennie Conroy, Trevor Doyle, Marthe Bryant-Genevier, Mercedes K. Taylor, Noel Southall, Xin Hu, Marc Ferrer, Steve Titus, Wei Zheng, David R. Sibley, Juan J. Marugan. | Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists | Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2012 Dec 25 [updated 2013 Sep 03]. |
Jung-eun Park, Wan Keun Ji, Jae Wan Jang, Ae Nim Pae, Keehyun Choi, Ki Hang Choi, Jahyo Kang, Eun Joo Roh | Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers | Bioorg Med Chem Lett. 2013 Mar 15;23(6):1887-90. doi: 10.1016/j.bmcl.2012.12.072. Epub 2013 Jan 12. |
Jutty Rajan Prashanth, Richard J. Lewis, Sebastien Dutertre | Towards an integrated venomics approach for accelerated conopeptide discovery | Toxicon. 2012 Sep 15;60(4):470-7. doi: 10.1016/j.toxicon.2012.04.340. Epub 2012 Apr 28. |
Linjie Chen, Lili Jin, Naiming Zhou | An update of novel screening methods for GPCR in drug discovery | Expert Opin Drug Discov. 2012 Sep;7(9):791-806. doi: 10.1517/17460441.2012.699036. Epub 2012 Jun 21. |
Mohammed Akhlaq; Elizabeth M. Rosethorne; Afrah Sattikar; Toby C. Kent | The Use of Cold Plasma Technology to Reduce Carryover in Screening Assays | J Lab Autom. 2013 Aug;18(4):269-75. doi: 10.1177/2211068212457780. Epub 2012 Sep 14. |
Nalin L. Subasinghe, Mark J. Wall, Michael P. Winters, Ning Qin, Mary Lou Lubin, Michael F.A. Finley, Michael R. Brandt, Michael P. Neeper, Craig R. Schneider, Raymond W. Colburn, Christopher M. Flores, Zhihua Sui | A novel series of pyrazolylpiperidine N-type calcium channel blockers | Bioorg Med Chem Lett. 2012 Jun 15;22(12):4080-3. doi: 10.1016/j.bmcl.2012.04.075. Epub 2012 May 2. |
Roman Hudec, Kozo Hamada, Katsuhiko Mikoshiba | A fluorescence-based assay for the measurement of S-adenosylhomocysteine hydrolase activity in biological samples | Anal Biochem. 2013 Feb 15;433(2):95-101. doi: 10.1016/j.ab.2012.10.014. Epub 2012 Oct 15. |
Shen Yin, Rocio Zamorano, P. Jeffrey Conn, Colleen M. Niswender | Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors | Neuropharmacology. 2013 Mar;66:122-32. doi: 10.1016/j.neuropharm.2012.03.003. Epub 2012 Mar 9. |
Shuzo Watanabe | Discovery of voltage-gated sodium-channel blockers for the treatment of neuropathic pain | Nihon Yakurigaku Zasshi. 2012 Nov;140(5):201-5. doi: 10.1254/fpj.140.201 |
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Yueming Zheng, Xuejing Zhu, Pingzheng Zhou, Xi Lan, Haiyan Xu, Min Li, Zhaobing Gao | Hexachlorophene Is a Potent KCNQ1/KCNE1 Potassium Channel Activator Which Rescues LQTs Mutants | PLoS One. 2012;7(12):e51820. doi: 10.1371/journal.pone.0051820. Epub 2012 Dec 12. |
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Atsushi Inayoshi, Yoshiyuki Sugimoto, Jun Funahashi, Saori Takahashi, Masahiro Matsubara, Hideaki Kusaka | Mechanism underlying the block of human Cav3.2 T-type Ca2+ channels by benidipine, a dihydropyridine Ca2+ channel blocker | Life Sci. 2011 May 9;88(19-20):898-907. doi: 10.1016/j.lfs.2011.03.019. Epub 2011 Apr 3. |
C. David Weaver | Triple-Addition Assay Protocols for Detecting and Characterizing Modulators of Seven-Transmembrane Receptors | Curr Protoc Chem Biol. 2011 Sep 1;3(3):119-40. doi: 10.1002/9780470559277.ch110060. |
Carrie K. Jones, Michael Bubser, Analisa D. Thompson, Jonathan W. Dickerson, Nathalie Turle-Lorenzo, Marianne Amalric, Anna L. Blobaum, Thomas M. Bridges, Ryan D. Morrison, Satyawan Jadhav, Darren W. Engers, Kimberly Italiano, Jacob Bode, J. Scott Daniels, Craig W. Lindsley, Corey R. Hopkins, P. Jeffrey Conn, Colleen M. Niswender | The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with L-DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease | J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16. |
Curtis A. Thorne, Bonnie Lafleur, Michelle Lewis, Alison J. Hanson, Kristin K. Jernigan, David C. Weaver, Kari A. Huppert, Tony W. Chen, Chonlarat Wichadiit, Christopher S. Cselenyi, Emilios Tahinci, Kelly C. Meyers, Emily Waskow, Darren Orton, Adrian Salic, Laura A. Lee, David J. Robbins, Stacey S. Huppert, Ethan Lee | A Biochemical Screen for Identification of Small-Molecule Regulators of the Wnt Pathway Using Xenopus Egg Extracts | J Biomol Screen. 2011 Oct;16(9):995-1006. doi: 10.1177/1087057111416657. Epub 2011 Aug 21. |
Gaelle Dintilhac, Deniz Arslan, Sebastien Dilly, Laurence Danober, Iuliana Botez, Pierre Lestage, Bernard Pirotte, Pascal de Tullio | New substituted aryl esters and aryl amides of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors | Med. Chem. Commun., 2011,2, 509-523 doi: 10.1039/C1MD00069A |
Haibo Yu, Meng Wu, Corey Hopkins, Julie Engers, Steve Townsend, Craig Lindsley, Owen B McManus, Min Li. | A small molecule activator of KCNQ2 and KCNQ4 channels. | Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Mar 29 [updated 2013 Feb 28]. |
Haibo Yu, Kaiping Xu, Beiyan Zou, Meng Wu, Owen B. McManus, Julie Le Engers, Yiu-Yin Cheung, James M. Salovich, Corey R. Hopkins, Craig W. Lindsley, and Min Li. | Identification of a novel, small molecule inhibitor of KCNQ2 channels | Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Oct 28 [updated 2013 Feb 25]. |
Haibo Yu, Zhihong Lin, Kaiping Xu, Xiaofang Huang, Shunyou Long, Meng Wu, Owen B. McManus, Julie Le Engers, Margrith E. Mattmann, Darren W. Engers, Uyen M. Le, Craig W. Lindsley, Corey R. Hopkins, Min Li. | Identification of a novel, small molecule activator of KCNQ1 channels | Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Dec 16 [updated 2013 Mar 7]. |
Jacques Pantela, Savannah Y. Williams, Dehui Mi, Julien Sebag, Jackie D. Corbin, C. David Weaver, Roger D. Cone | Development of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay | Eur J Pharmacol. 2011 Jun 11;660(1):139-47. doi: 10.1016/j.ejphar.2011.01.031. Epub 2011 Feb 4. |
Jinghai Song, Hiroshi Hagiya, Haruto Kurata, Hirotaka Mizuno, Toshinori Ito | Prevention of GVHD and graft rejection by a new S1P receptor agonist, W-061, in rat small bowel transplantation | Transpl Immunol. 2012 Mar;26(2-3):163-70. doi: 10.1016/j.trim.2011.12.005. Epub 2011 Dec 14. |
Jun Chen, Regina M. Reilly, Philip R. Kym, and Shailen Joshi. | In Vitro and in Vivo Assays for the Discovery of Analgesic Drugs Targeting TRP Channels | In: Zhu MX, editor. TRP Channels. Boca Raton (FL): CRC Press; 2011. Chapter 18. |
Marianthi Papakosta, Carine Dalle, Alison Haythornthwaite, Lishuang Cao, Edward B. Stevens, Gillian Burgess, Rachel Russell, Peter J. Cox, Stephen C. Phillips, Christian Grimm | The Chimeric Approach Reveals That Differences in the TRPV1 Pore Domain Determine Species-specific Sensitivity to Block of Heat Activation | J Biol Chem. 2011 Nov 11;286(45):39663-72. doi: 10.1074/jbc.M111.273581. Epub 2011 Sep 12. |
Menghang Xia, Sampada A. Shahane, Ruili Huang, Steven A. Titus, Enoch Shum, Yong Zhao, Noel Southall, Wei Zheng, Kristine L. Witt, Raymond R. Tice, Christopher P. Austin | Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channels | Toxicol Appl Pharmacol. 2011 May 1;252(3):250-8. doi: 10.1016/j.taap.2011.02.016. Epub 2011 Feb 26. |
Meredith J Noetzel, Jerri M Rook, Paige N Vinson, Hyekyung Cho, Emily Days, Y Zhou, Alice L Rodriguez, Hilde Lavreysen, Shaun R Stauffer, Colleen M Niswender, Zixiu Xiang, J Scott Daniels, Crag W Lindsley, C David Weaver, P Jeffrey Conn | Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of mGlu5 in Regulating CNS Function | Mol Pharmacol. 2012 Feb;81(2):120-33. doi: 10.1124/mol.111.075184. Epub 2011 Oct 21. |
Peter R McDonald, Anuradha Roy, Rathnam Chaguturu | The University of Kansas High-Throughput Screening Laboratory. Part II: enabling collaborative drug-discovery partnerships through cutting-edge screening technology | Future Med Chem. 2011 Jul;3(9):1101-10. doi: 10.4155/fmc.11.84. |
Rene Raphemot, Daniel F. Lonergan, Thuy T. Nguyen, Thomas Utley, L. Michelle Lewis, Rishin Kadakia, C. David Weaver, Rocco Gogliotti, Corey Hopkins, Craig W. Lindsley, Jerod S. Denton | Discovery, characterization, and structure—activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.X, and Kir7.1 | Front Pharmacol. 2011 Nov 30;2:75. doi: 10.3389/fphar.2011.00075. eCollection 2011. |
Thierry Ferain, Hamid Hoveyda, Frederic Ooms, Dominique Schols, Jerome Bernard, Graeme Fraser | Agonist-Induced Internalization of CC Chemokine Receptor 5 as a Mechanism to Inhibit HIV Replication | J Pharmacol Exp Ther. 2011 Jun;337(3):655-62. doi: 10.1124/jpet.111.179622. Epub 2011 Mar 9. |
Xinmin Xie, John T. Brogan, Michael L. Schulte, Debbie Mi, Haibo Yu, Eric S. Dawson, Min Li, Owen McManus, Julie Engers, L. Michelle Lewis, Analisa Thompson, Carrie K. Jones, C. David Weaver, Craig W. Lindsley. | Scaffold Hopping Affords a Highly Selective in vitro and in vivo T-Type Calcium Inhibitor Probe Free From IP Issues | Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. 2011 Mar 31 [updated 2013 Mar 22]. |
Yasuaki Sanada, Tsunekazu Mizushima, Yasuyuki Kai, Junichi Nishimura, Hiroshi Hagiya, Haruto Kurata, Hirotaka Mizuno, Etsuko Uejima, Toshinori Ito | Therapeutic Effects of Novel Sphingosine-1-Phosphate Receptor Agonist W-061 in Murine DSS Colitis | PLoS One. 2011;6(9):e23933. doi: 10.1371/journal.pone.0023933. Epub 2011 Sep 8. |
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Ke Liu, Noel Southall, Steve A. Titus, James Inglese, Robert L. Eskay, Paul Shinn, Christopher P. Austin, Markus A. Heilig and Wei Zheng. | A Multiplex Calcium Assay for Identification of GPCR Agonists and Antagonists | Assay Drug Dev Technol. 2010 Jun;8(3):367-79. |
Brad P. Barnett, Yousang Hwang, Martin S. Taylor, Henriette Kirchner, Paul T. Pfluger, Vincent Bernard, Yu-yi Lin, Erin M. Bowers, Chandrani Mukherjee, Woo-Jin Song, Patti A. Longo, Daniel J. Leahy, Mehboob A. Hussain, Matthias H. Tschop, Jef D. Boeke and Philip A. Cole. | Glucose and Weight Control in Mice with a Designed Ghrelin O-Acyltransferase Inhibitor | Science 17 December 2010: Vol. 330 no. 6011 pp. 1689-1692. |
Evan P Lebois, Thomas M Bridges, L. Michelle Lewis, Eric S Dawson, Alexander S. Kane, Zixiu Xiang, Satyawan B Jadhav, Huiyong Yin, J. Phillip Kennedy, Jens Meiler, Colleen M. Niswender, Carrie K Jones, P Jeffrey Conn, C David Weaver, and Craig W Lindsley. | Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system | ACS Chem Neurosci. 2010; 1(2): 104-121. |
Zhaobing Gao, Tangzhi Zhang, Meng Wu, Qiaojie Xiong, Haiyan Sun, Yinan Zhang, Liansuo Zu, Wei Wang and Min Li | Isoform-specific Prolongation of Kv7 (KCNQ) Potassium Channel Opening Mediated by New Molecular Determinants for Drug-Channel Interactions | September 3, 2010 The Journal of Biological Chemistry, 285, 28322-28332. |
Jinliang Sui, Shakira Cotard, Jennifer Andersen, Ping Zhu, Jane Staunton, Margaret Lee, and Stephen Lin. | Optimization of a Yellow Fluorescent Protein-Based Iodide Influx High-Throughput Screening Assay for Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Modulators | ASSAY and Drug Development Technologies. December 2010, 8(6): 656-668. doi:10.1089/adt.2010.0312. |
Stephen Lin, Jinliang Sui, Shakira Cotard, Brenda Fung, Jennifer Andersen, Ping Zhu, Najib El Messadi, Joseph Lehar, Margaret Lee, and Jane Staunton. | Identification of Synergistic Combinations of F508del Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Modulators | ASSAY and Drug Development Technologies. December 2010, 8(6): 669-684. doi:10.1089/adt.2010.0313. |
Authors | Title | Source |
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Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD. | Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2 | Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. Epub 2009 Mar 11. |
Irukayama-Tomobe Y, Tanaka H, Yokomizo T, Hashidate-Yoshida T, Yanagisawa M, Sakurai T. | Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B | Proc Natl Acad Sci U S A. 2009 Mar 10;106(10):3930-4. Epub 2009 Feb 23. |
Lewis LM, Bhave G, Chauder BA, Banerjee S, Lornsen KA, Redha R, Fallen K, Lindsley CW, Weaver CD, Denton JS. | High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1 | Mol Pharmacol. 2009 Nov;76(5):1094-103. Epub 2009 Aug 25. |
Marlo JE, Niswender CM, Days EL, Bridges TM, Xiang Y, Rodriguez AL, Shirey JK, Brady AE, Nalywajko T, Luo Q, Austin CA, Williams MB, Kim K, Williams R, Orton D, Brown HA, Lindsley CW, Weaver CD, Conn PJ. | Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity | Mol Pharmacol. 2009 Mar;75(3):577-88. Epub 2008 Dec 1. |
Sheffler DJ, Williams R, Bridges TM, Xiang Z, Kane AS, Byun NE, Jadhav S, Mock MM, Zheng F, Lewis LM, Jones CK, Niswender CM, Weaver CD, Lindsley CW, Conn PJ. | A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning | Mol Pharmacol. 2009 Aug;76(2):356-68. Epub 2009 Apr 30. |
Shirey JK, Brady AE, Jones PJ, Davis AA, Bridges TM, Kennedy JP, Jadhav SB, Menon UN, Xiang Z, Watson ML, Christian EP, Doherty JJ, Quirk MC, Snyder DH, Lah JJ, Levey AI, Nicolle MM, Lindsley CW, Conn PJ. | A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning | J Neurosci. 2009 Nov 11;29(45):14271-86. |
Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. | Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins | J Med Chem. 2009 Jun 11;52(11):3445-8. |
Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. | Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs) | J Med Chem. 2009 Jul 23;52(14):4115-8. |
Sharma S, Kedrowski J, Rook JM, Smith RL, Jones CK, Rodriguez AL, Conn PJ, Lindsley CW. | Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines | J Med Chem. 2009 Jul 23;52(14):4103-6. |
Wise H, Abel PW, Cawkill D. | Use of reduced temperature cell pausing to enhance flexibility of cell-based assays | J Biomol Screen. 2009 Jul;14(6):716-22. Epub 2009 May 21. |
Mori T, Itami S, Yanagi T, Tatara Y, Takamiya M, Uchida T. | Use of a real-time fluorescence monitoring system for high-throughput screening for prolyl isomerase inhibitors | J Biomol Screen. 2009 Apr;14(4):419-24. |
Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, Conn PJ, Lindsley CW. | Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe | Curr Top Med Chem. 2009;9(13):1217-26. |
Kim Y, Kang S, Lee JY, Rhim H. | High throughput screening assay of alpha(1G) T-type Ca2+ channels and comparison with patch-clamp studies | Comb Chem High Throughput Screen. 2009 Mar;12(3):296-302. |
Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR. | Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4) | Bioorg Med Chem Lett. 2009 Sep 1;19(17):4967-70. Epub 2009 Jul 18. |
Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver CD, Conn PJ, Lindsley CW. | Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype | Bioorg Med Chem Lett. 2009 Jun 15;19(12):3209-13. Epub 2009 May 3. |
Williams R, Niswender CM, Luo Q, Le U, Conn PJ, Lindsley CW. | Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead | Bioorg Med Chem Lett. 2009 Feb 1;19(3):962-6. Epub 2008 Dec 25. |
Felts AS, Saleh SA, Le U, Rodriguez AL, Weaver CD, Conn PJ, Lindsley CW, Emmitte KA. | Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5 | Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6. Epub 2009 Oct 9. |
Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW. | Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS | Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6. Epub 2009 Oct 28. |
Titus SA, Beacham D, Shahane SA, Southall N, Xia M, Huang R, Hooten E, Zhao Y, Shou L, Austin CP, Zheng W. | A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel | Anal Biochem. 2009 Nov 1;394(1):30-8. Epub 2009 Jul 5. |
Lin Tian, S. Andrew Hires, Tianyi Mao, Daniel Huber, M. Eugenia Chiappe, Sreekanth H. Chalasani, Leopoldo Petreanu, Jasper Akerboom, Sean A. McKinney, Eric R. Schreiter, Cornelia I. Bargmann, Vivek Jayaraman, Karel Svoboda, and Loren L. Looger | Imaging neural activity in worms, flies and mice with improved GCaMP calcium indicators | "Nat Methods. 2009 December; 6(12): 875-881.Published online 2009 November 8. doi: 10.1038/nmeth.1398" |
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Taniguchi Y, Tonai-Kachi H, Shinjo K. | 5-Nitro-2-(3-phenylpropylamino)benzoic acid is a GPR35 agonist | Pharmacology. 2008;82(4):245-9. Epub 2008 Sep 26. |
Ayala JE, Niswender CM, Luo Q, Banko JL, Conn PJ. | Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated | Neuropharmacology. 2008 Apr;54(5):804-14. Epub 2007 Dec 24. |
Shirey JK, Xiang Z, Orton D, Brady AE, Johnson KA, Williams R, Ayala JE, Rodriguez AL, Wess J, Weaver D, Niswender CM, Conn PJ. | An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission | Nat Chem Biol. 2008 Jan;4(1):42-50. Epub 2007 Dec 2. |
Niswender CM, Johnson KA, Weaver CD, Jones CK, Xiang Z, Luo Q, Rodriguez AL, Marlo JE, de Paulis T, Thompson AD, Days EL, Nalywajko T, Austin CA, Williams MB, Ayala JE, Williams R, Lindsley CW, Conn PJ. | Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4 | Mol Pharmacol. 2009 Mar;75(3):577-88. Epub 2008 Dec 1. |
Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD. | A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors | Mol Pharmacol. 2008 Apr;73(4):1213-24. Epub 2008 Jan 2. |
Kobayashi K, Nishizawa Y, Sawada K, Ogura H, Miyabe M. | K(+)-channel openers suppress epileptiform activities induced by 4-aminopyridine in cultured rat hippocampal neurons | J Pharmacol Sci. 2008 Dec;108(4):517-28. Epub 2008 Dec 11. |
Jones CK, Brady AE, Davis AA, Xiang Z, Bubser M, Tantawy MN, Kane AS, Bridges TM, Kennedy JP, Bradley SR, Peterson TE, Ansari MS, Baldwin RM, Kessler RM, Deutch AY, Lah JJ, Levey AI, Lindsley CW, Conn PJ. | Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats | J Neurosci. 2008 Oct 8;28(41):10422-33. |
Akasofu S, Sawada K, Kosasa T, Hihara H, Ogura H, Akaike A. | Donepezil attenuates excitotoxic damage induced by membrane depolarization of cortical neurons exposed to veratridine | Eur J Pharmacol. 2008 Jul 7;588(2-3):189-97. Epub 2008 Apr 13. |
Gunnet JW, Wines P, Xiang M, Rybczynski P, Andrade-Gordon P, de Garavilla L, Parry TJ, Cheung WM, Minor L, Demarest KT, Maryanoff BE, Damiano BP. | Pharmacological characterization of RWJ-676070, a dual vasopressin V(1A)/V(2) receptor antagonis | Eur J Pharmacol. 2008 Aug 20;590(1-3):333-42. Epub 2008 Jun 7. |
Kim HJ, Yun HM, Kim T, Nam G, Roh EJ, Kostenis E, Choo HY, Pae AN, Rhim H. | Functional human 5-HT6 receptor assay for high throughput screening of chemical ligands and binding proteins | Comb Chem High Throughput Screen. 2008 May;11(4):316-24. |
Niswender CM, Lebois EP, Luo Q, Kim K, Muchalski H, Yin H, Conn PJ, Lindsley CW. | Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators | Bioorg Med Chem Lett. 2008 Oct 15;18(20):5626-30. Epub 2008 Aug 29. |
Lewis LM, Sheffler D, Williams R, Bridges TM, Kennedy JP, Brogan JT, Mulder MJ, Williams L, Nalywajko NT, Niswender CM, Weaver CD, Conn PJ, Lindsley CW. | Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists | Bioorg Med Chem Lett. 2008 Feb 1;18(3):885-90. Epub 2008 Jan 4. |
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Hemstapat K, Da Costa H, Nong Y, Brady AE, Luo Q, Niswender CM, Tamagnan GD, Conn PJ. | A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors | J Pharmacol Exp Ther. 2007 Jul;322(1):254-64. Epub 2007 Apr 6. |
Song F, Lu S, Gunnet J, Xu JZ, Wines P, Proost J, Liang Y, Baumann C, Lenhard J, Murray WV, Demarest KT, Kuo GH. | Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists | J Med Chem. 2007 Jun 14;50(12):2807-17. Epub 2007 May 15. |
Cassutt KJ, Orsini MJ, Abousleiman M, Colone D, Tang W. | Identifying nonselective hits from a homogeneous calcium assay screen | J Biomol Screen. 2007 Mar;12(2):285-7. Epub 2007 Feb 8. |
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