Guiding Medicinal Chemistry with Pharmacology in an Allosteric World

Friday, March 25, 2011
11:30 a.m. - 1:00 p.m. EST


Course Description:
This module of the course begins with a discussion of the current model for functional allosteric modulation in receptors and the three basic types of allosteric molecule of therapeutic interest: PAMs (Positive Allosteric Modulators), Allosteric Antagonists, and Allosteric Agonists. To completely characterize an allosteric molecule, three parameters must be estimated: a (effect on affinity), b (effect on efficacy) and tB (direct agonist effect). This module will discuss specific methods to do this. In addition, special considerations required for allosteric screens will be discussed.

Learning Objectives:
This session is designed to solve a problem, namely the use of the functional models of allosteric function to characterize molecules in a system independent manner with parameters that are applicable to all systems and which can be used to predict allosteric effect in all systems.

This module also will discuss how to optimize assays for the discovery of (screening) and characterization  (lead optimization ) of allosteric molecules


Instructor Information: 
Terry KenakinTerry Kenakin Ph.D.
Professor, Department of Pharmacology
University of North Carolina School of Medicine
Chapel Hill NC

Instructor Biography:
Terrence Kenakin, Ph.D., is Professor in the Department of Pharmacology, University of North Carolina, Chapel Hill. Until August of 2011, Dr. Kenakin was director of research at GlaxoSmithKline Research and Development laboratories at Research Triangle Park, NC where he optimized drug activity assay systems for the discovery and testing of. allosteric molecules mostly for the treatment of diabetes. Before starting the major stint of his drug discovery career at GSK, Dr. Kenakin was an associate scientist at Burroughs-Wellcome in the U.K. which he joined after a post-doctoral fellowship at University College London, U.K. Dr. Kenakin earned his Ph.D. in Pharmacology at the University of Alberta, Edmonton Canada.

Dr. Kenakin is a member of many editorial boards as well as Co-editor-in-Chief of the Journal of Receptors and Signal Transduction. In addition, he has authored numerous articles and has written eight books on pharmacology, including the popular "A Pharmacology Primer".

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