2024年培训研讨会（仅限到场参加）
Campbridge HealthTech Institute的培训研讨会涵盖了广泛的学术理论和背景，以及现实世界的案例研究、遇到的问题和应用解决方案。 每个培训研讨会将正式讲座与互动讨论和行动相结合，以最大限度地提高学习体验。 培训研讨会由经验丰富的讲师主持，重点关注适用于当前研究的内容，同时也为该领域的新手提供重要指导。
药物化学训练研讨会仅以现场形式举行。
2024 年 4 月 2 日星期二 8:00 AM - 3:20 PM | 2024 年 4 月 3 日星期三 8:30 AM - 12:00 PM
TS1: The Medicinal Chemistry-Pharmacology Interface:
The 3 Independent SARs for New Drug Candidates
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.
Training Seminar Information
Though CHI encourages track hopping between conference programs, we ask that Training Seminars not be disturbed once they have begun. In the interest of maintaining the highest quality learning environment for Training Seminar attendees, and because seminars are conducted differently than conference programming, we ask that attendees commit to attending the entire program, and not engage in track hopping, as to not disturb the hands-on style instruction being offered to the other participants.
* 活动内容有可能不事先告知作更动及调整。
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