Cambridge Healthtech Instituteのトレーニングセミナーでは、実際のケーススタディ、直面した問題および適用された解決策、学術的な理論と背景に関する広範な情報が提供されます。各トレーニング セミナーでは、学習体験を最大化するために、公式の講義とインタラクティブなディスカッションおよびアクティビティを組み合わせて提供します。 これらのトレーニングセミナーは、経験豊富なインストラクターが指導し、現在の研究に適用できる内容に焦点を当て、その分野に不慣れな人への重要なガイダンスを提供します。


2023年9月27日(水) 午後1:45〜5:00 | 2023年9月28日 午前8:00〜午後4:20

TS1: The Renaissance in GPCRs as Drug Targets: Allosteric Function and Biased Signaling

This training seminar describes models and tools that extend GPCR pharmacology into new therapeutic areas. I review functional assays and concepts guiding molecular dynamic simulations and their impact on GPCR allosteric function and biased agonism, focusing on allosteric screening and allosteric functional and binding models. Coverage emphasizes characterization of Biased Agonists, Positive Allosteric Modulators (PAMs), and Negative Allosteric Modulators (NAMs) in practical terms for application to drug discovery.

Section 1:

  • Zero to hero: the revitalization of GPCRs as drug targets
  • GPCRs as nature’s prototype allosteric protein: allosteric mechanism(s)
  • GPCR families: established and uncharted territory
  • Models of GPCR function: functional allosteric model, Black/Leff operational model
  • The impact of molecular dynamics

Section 2:

  • GPCR druggability: technologies for finding ligands
  • Allosteric screens: another shot on goal
  • The unique properties of allosteric modulators: efficacy 
  • Quantifying the power to induce response

Section 3:

  • Biased signaling: methods to measure and quantify it
  • Determining and quantifying allosteric parameters (a, b, tB)NAMs and PAMs applied to drug therapy
  • PAM-antagonists: a better way to block response


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.

* 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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