2023 ARCHIVES

OVERVIEW
DOWNLOAD BROCHURE
TESTIMONIALS
GROUP DISCUSSIONS
SHORT COURSES
TRAINING SEMINARS
PLENARY KEYNOTES
ATTENDEES
NETWORKING

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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.


Training Seminar will be offered IN-PERSON ONLY.

Wednesday, September 27, 2023  1:45 - 5:00 pm | Thursday, September 28, 2023  8:00 am - 4:20 pm

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.
Terrence P. Kenakin, PhD, Professor, Pharmacology, University of North Carolina at Chapel Hill

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

INSTRUCTOR BIOGRAPHIES:

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.