2024年培訓研討會(僅限到場參加)

Campbridge HealthTech Institute的培訓研討會涵蓋了廣泛的學術理論和背景,以及現實世界的案例研究、遇到的問題和應用解決方案。 每個培訓研討會將正式講座與互動討論和行動相結合,以最大限度地提高學習體驗。 培訓研討會由經驗豐富的講師主持,重點關注適用於當前研究的內容,同時也為該領域的新手提供重要指導。

藥物化學訓練研討會僅以現場形式舉行。

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. KenakinTerrence 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.


* 活動內容有可能不事先告知作更動及調整。

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