Quantifying Receptor Activation and Agonism: Why Measuring Only Potency Falls Short

October 29, 2012
12:00 p.m. - 1:30 p.m. EDT



Course Description

The potency of activating drugs varies tremendously in different cells making measures of absolute potency for predicting therapeutic of very limited value. This session discusses how dose-response curves can be reduced to cell-type independent parameters describing the molecular properties of affinity and efficacy through application of the Black/Leff operational model of agonism. Biased agonism also is discussed in terms of the assays and parameters that can be used to determine functionally selective effect. This lecture will equip the student to quantify agonist activity in a test system and be able to predict activity of the agonist in all systems.

  • This session is designed to solve a problem, namely that of using in vitro agonist potency data to predict agonism in all systems including the therapeutic one.
  • Methods to detect functional selectivity and what this effect might mean to therapeutically relevant agonism also will be discussed.
  • Students will be able to apply the Black/Leff operational model to quantify agonism.

Who Should Attend:

  • Any biological scientist dealing with dose-response data in integrated systems (pharmacologists, biochemists, enzymologists)
  • Medicinal chemists who must understand dose-response data



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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