Cambridge Healthtech Institute Training Seminars offer real-life case studies, problems encountered, and solutions applied, along with extensive coverage of the academic theory and background. Each training seminar offers a mix of formal lecture and interactive discussions and activities to maximize the learning experience. These training seminars are led by experienced instructors who will focus on content applicable to your current research and provide important guidance for those new to their fields.
TUESDAY, APRIL 2, 2024 8:00 AM - 3:20 PM | WEDNESDAY, APRIL 3, 2024 8:30 AM - 12:00 PM
This training seminar will cover the three independent structure-activity-relationships (SARs) that must be satisfied for new drug success: (1) Primary Target Activity, (2) Pharmacokinetic Profile, and (3) Safety.
Seminar Outline:
Day 1 (AM): SAR 1: Primary Target Activity
- (a) Affinity: What concentrations are needed in the receptor compartment for target binding?
- (b) Efficacy: How do drugs produce cellular response (drugs have many efficacies)? How the combination of signaling effects yields a ‘quality’ of efficacy to cells.
Day 1 (PM): SAR 1: Primary Target Activity (cont.)
- Efficacy/how biased-signaling causes complex patterns of efficacy (and how can this be manipulated?)
- Allosteric vs. orthosteric interaction of molecules: how allosteric interaction fundamentally differs from orthosteric (same site) interaction
- Kinetics of ligand interaction for in vivo target coverage: the importance of in vivo-restricted diffusion/importance of receptor offset rates for target coverage (PK-PD dissociation)/methods to measure kinetics
Day 2 (AM): SAR 2-Pharmacokinetic Profile and SAR 3—Safety
- SAR 2 (ADME): Methods for modification of candidate ADME properties (modification of ‘druglike’ activity/specific modification of interactions with recognition processes (i.e., hepatic enzymes, transporters)
- SAR 3: Safety: Basic safety issues faced early on (cytotoxicity, hepatotoxicity, hERG, Ames test)/translation of in vitro to in vivo activity
INSTRUCTOR BIOGRAPHY:
Terrence P. Kenakin, PhD, Professor, Pharmacology, University of North Carolina at Chapel Hill
Beginning his career as a synthetic chemist, Terry Kenakin received a PhD in Pharmacology at the University of Alberta in Canada. After a postdoctoral fellowship at University College London, UK, he joined Burroughs-Wellcome as an associate scientist for 7 years. From there, he continued working in drug discovery for 25 years first at Glaxo, Inc., then Glaxo Wellcome, and finally as a Director at GlaxoSmithKline Research and Development laboratories at Research Triangle Park, North Carolina, USA. Dr. Kenakin is now a professor in the Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill. Currently he is engaged in studies aimed at the optimal design of drug activity assays systems, the discovery and testing of allosteric molecules for therapeutic application, and the quantitative modeling of drug effects. In addition, he is Director of the Pharmacology graduate courses at the UNC School of Medicine. He is a member of numerous editorial boards, as well as Editor-in-Chief of the “Journal of Receptors and Signal Transduction.” He has authored numerous articles and has written 10 books on pharmacology.