トレーニングセミナー | 19th Annual Drug Discovery Chemistry 2024 公式サイト

2024年度トレーニングセミナー（対面参加のみ）

Cambridge Healthtech Instituteのトレーニングセミナーでは、学術的理論やその背景事情を幅広くカバーするとともに、実際の事例研究や、直面した課題と適用した解決策などについて説明します。各セミナーは、正式な講義と対話型ディスカッション・活動を取り交ぜて、学習体験を最大化できるようになっています。このトレーニングセミナーでは経験豊富な講師が司会者となり、ご自分の現在の研究に適用可能な内容に焦点を合わせ、またこの分野を初めて学ぶ人にも重要なガイダンスを提供します。

Drug Discovery Chemistryのトレーニングセミナーは対面形式でのみ開催されます。

2024年4月2日（火） 8:00 AM - 3:20 PM | 2024年4月3日（水） 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.

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.

* 不測の事態により、事前の予告なしにプログラムが変更される場合があります。

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