2013 Archived Content

SC9 PHARMACOLOGY AND DRUG DISCOVERY IN THE ALLOSTERIC WORLD 

Monday, February 20, 2012 | 1:00 – 4:00 PM

Course Instructor: Terry Kenakin, Ph.D., Professor, Department of Pharmacology, University of North Carolina

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".

Course Overview:


The advancing technology of high-throughput screening is changing the type of molecules found. With protein function more physiologically relevant, the quality of the molecules that pharmacologists and medicinal chemists must deal with is changing. This course will familiarize researchers with the tools needed to exploit this potentially fruitful area of new drug discovery through discussion of allosteric molecules, detection of allosterism, and quantifying allosterism for chemical lead optimization.

The course is designed to answer these questions:

  • What is protein allostery?
  • What makes allosteric molecules unique and how can this contribute to unique therapeutic properties?
  • How can we detect allosterism?
  • How to quantify allosterism for chemical lead optimization?
 

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