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基于GPCR的创药 2011年11月2日 星期三 7:00 am Conference Registration and Morning Coffee ligand bias信号传达 8:30 Chairperson’s Opening Remarks Annette Gilchrist, Ph.D., Assistant Professor, Department of Pharmaceutical Sciences, Midwestern University
9:40 GPCR Biased Ligands: Translating Theory to Improved Therapies Jonathan Violin, Ph.D., Head of Biology, Trevena Biased GPCR ligands selectively engage or elude distinct receptor signaling mechanisms, and may provide a strategy for designing safer and more efficacious GPCR-targeted drugs. Two examples illustrate how biased ligands can elicit novel pharmacological profiles: TRV027, a beta-arrestin biased ligand of angiotensin II type 1 receptor, and TRV002, a G protein-biased ligand of the mu opioid receptor. These compounds highlight the concept, mechanism of action, and utility of biased ligands. 10:10 Grand Opening Coffee Break in the Exhibit Hall with Poster Viewing
GPCR筛选的课题 10:40 Talk Title to be Announced Mark Pausch, Ph.D., Director, in vitro Pharmacology, Merck 11:10 Sponsored Presentations (Opportunities Available) 11:40 Hit Identification and Hit Assessment for the Orphan G Protein-Coupled Receptor GPR88 Neil Burford, Ph.D., Senior Research Investigator II, Lead Discovery & Profiling, Bristol-Myers Squibb Company GPR88 is highly expressed in brain regions and is implicated in the modulation of striatal dopamine function. GPR88 knockout mice exhibit a pro-psychotic behavioral phenotype suggesting that GPR88 agonists might be therapeutically beneficial as a treatment for schizophrenia. In this case study, the discovery of surrogate agonists for GPR88 from high throughput screening will be described with emphasis on the challenges associated with screening an orphan GPCR. 12:10 pm Panel Discussion: Which Screening Strategy to Use? Moderator: Lisa K. Minor, Ph.D., President, In vitro Strategies, LLC Panelists will present their screening strategy and choice of assays in response to vaious mock drug discovery scenarios presented by the moderator. Sponsored by Discovery of Novel, Biased Ligands Using a Suite of PathHunter® and HitHunter® GPCR Screening Platforms Elizabeth R. Quinn, Ph.D., Senior Product Manager, GPCR Product Portfolio, DiscoveRx Corp. Although G-protein dependent and independent pathways are often modulated in concert, a number of compounds having differential effects on these pathways have been reported. In order to gain further insight into this, a systematic characterization of GPCR targets and their associated ligands was done using: HitHunter® 2nd messenger signaling, PathHunter® arrestin activation, and PathHunter® receptor internalization. This talk focuses on how functional selectivity may be prevalent across receptor and ligand classes which could lead into discovery of compounds with novel characteristics. 信号传达复合体 2:20 Chairperson’s Remarks 2:25 Talk Title to be Announced Thue Schwartz, Ph.D., Professor, The Novo-Nordisk Foundation Center for Basic Metabolic Research, University of Copenhagen 2:55 Regulators of Heterotrimeric G-protein Signaling David Siderovski, Ph.D., Professor, Director, Chemical Biology, Department of Pharmacology, University of North Carolina at Chapel Hill I discuss two distinct families of GPCR signaling modulators discovered in my laboratory: the ‘regulators of G-protein signaling’ (RGS) and GoLoco motif protein families. I will survey some of our latest findings on the physiological functions of RGS proteins and examine recent efforts to establish and validate proof-of-principle small molecule modulators of these proteins. 3:25 Networking Refreshment Break in the Exhibit Hall with Poster Viewing 4:05 Antiparkinsonian and Anxiolytic Effects of a Novel Chemical Class of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 Brice Campo, Ph.D., Group Leader, In vitro Pharma, Addex Addex will disclose a novel chemical scaffold with a pharmacophore and structure activity relationship that is completely different from what it’s known in the field. We also describe a proof-of-concept compound demonstrating efficacy in pre-clinical models of PD and anxiety disorders without any side effects(dyskenisias)associated with the existing frontline therapy l-DOPA. This work has been done in collaboration with Merck. 4:35 Generating Fully Human Antagonistic Antibodies against GPCR Targets Sergej Kiprijanov, Ph.D., Vice President of Research and Preclinical Development, Affitech A/S Using proprietary CBAS™ technology, Affitech generated a panel of antagonistic antibodies against GPCR targets involved in cancer progression and inflammation. The generated antibodies effectively competed with ligand binding, were able to block ligand-induced signaling and cell migration, and demonstrated high cell killing activity via ADCC. Data showing applicability of the GPCR targeting antibodies for treatment of cancer, inflammatory and autoimmune diseases will be presented. 5:05 Interactive Breakout Discussion Groups 6:15 – 7:15 Welcoming Reception in the Exhibit Hall with Poster Viewing
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