International Chair of Therapeutic Innovation Member Laboratories: Cea iBiTec-S SCBM Cea iBiTec-S SIMOPRO Cea iBiTec-S SPI Cnrs UMR 8076 Cnrs UMR 8113 Cnrs UMR 8122 Cnrs UMR 8182 Cnrs UMR 8612 Cnrs UPR 2301 Inserm UMR-S 1180 Inserm UMR-S 914 Inserm UMR-S 981 Inserm UMR-S 996 Inserm UMR-S 999 Inserm UMR-S 1184 Inserm UMR-S 1030 Coordinating Partner: PLENARY LECTURE Partner Institutions: by Professor Brian SHOICHET Department of Pharmaceutical Chemistry, University of California, San Francisco, United States Date : Vendredi 15 janvier 2016 à 14h30 Lieu : Contact: Dr. Rodolphe Fischmeister Coordinator LabEx LERMIT Inserm UMR-S 1180 Faculté de Pharmacie Université Paris-Sud 5, Rue Jean-Baptiste Clément 92296 Châtenay-Malabry Cedex France Tel.: +33-1-46.83.57.71 Fax: +33-1-46.83.54.75 rodolphe.fischmeister@inserm.fr www.labex-lermit.fr Amphithéâtre CHEMLA, Bâtiment IDA Ecole Normale Supérieure de Cachan 61 Avenue du Président Wilson, 94230 Cachan http://www.ens-cachan.fr/versionfrancaise/outils/plan-d-acces/plan-d-acces53.kjsp?RH=1266220367141 Contact : aurelie.lando@u-psud.fr International Chair of Therapeutic Innovation Prof. Brian Shoichet Department of Pharmaceutical Chemistry, University of California, San Francisco, United States Pr. Brian Shoichet received a B.Sc. in Chemistry and a B.Sc. in History in 1985, from MIT. He received his Ph.D. for work with Tack Kuntz on molecular docking in 1991, from UCSF. Shoichet's postdoctoral research focused on protein structure and stability with Brian Matthews at the Institute of Molecular Biology in Eugene, Oregon. In 1996, Pr. Shoichet joined the Dept. of Molecular Pharmacology & Biological Chemistry of Northwestern University as an Assistant Professor. In 2002, Pr. Shoichet was promoted to a tenured Associate Professor. Around that time he was recruited back to UCSF, where he is now a Professor in the Department of Pharmaceutical Chemistry. Research in Pr. Shoichet’s Lab seeks to bring chemical reagents to biology, combining computational simulation and experiment. An unanticipated observation emerging from the theory/experiment cycle was the colloidal aggregation of organic molecules. This phenomenon has great effects in early and late drug discovery, and remains under investigation. More broadly, the Schoichet Lab adopts a protein-centric approach that seeks new ligands to complement protein structures. This involves development of new docking methods and experimental model systems to test them. Using a ligand-centric approach, the Shoichet Lab seeks new targets for established drugs and reagents. Whereas this lacks the physical foundation of the structure-based research program, it returns to an older, pharmacological view of biological relationships, bringing to it a quantitative model. A focus for both approaches is ligand discovery against G Protein-Coupled Receptors (GPCRs). Publications MJ Keiser et al. Predicting new molecular targets for known drugs. Nature, 462, 175-81 (2009). J Carlsson et al. Comparing structure-based ligand discovery from a homology model and the crystal structure of the dopamine D3 receptor. Nature Chem. Biol. 7, 769-78 (2011). C Laggner, et al. Chemical Informatics and Target Identification in a Zebrafish Phenotypic Screen. Nature Chem. Biol., 8, 144-146 (2012). E Lounkine et al. Large Scale Prediction and Testing of Drug Activity on Side-Effect Targets. Nature 486, 361-7. (2012). H Lin et al. A Pharmacological Organization of G Protein-coupled Receptors. Nature Methods 10, 140-6 (2013). London et al. Covalent docking of large libraries for the discovery of chemical probes. Nature Chem Biol. 10, 1066-72 (2014). XP Haung et al. Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65. Nature in press (2015). Website: http://www.bkslab.org/index.php Video: Pr. Shoichet, channeling William F. Buckley, offers a vigorous defense of docking and highthroughput screening for the graduate student retreat (interviewed by Emily Crawford, channeling Steven Colbert).
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