Introduction
GPCR signaling kinetics, the temporal dynamics of receptor activation and downstream signaling, directly influence therapeutic outcomes from beta-agonist tachyphylaxis to opioid tolerance. This session addresses the clinical landscape of kinetic-dependent drug action, biosensor-based measurement of signaling over time, and analytical approaches for extracting actionable kinetic parameters in drug discovery.
Coverage spans tachyphylaxis mechanisms in beta-agonist therapy, tolerance development with opioid agonists, and therapeutic desensitization strategies at S1P1 and GnRH receptors. Designed for pharmacologists, drug discovery scientists, and translational researchers working on temporal aspects of GPCR therapeutics.
Instructor
Sam Hoare is a drug discovery consultant and founder of Pharmechanics LLC, specializing in kinetic analysis of drug action and the application of binding and signaling kinetics to therapeutic development.
After completing his Ph.D. in biochemistry studying allosteric modulation of dopamine receptors at the University of Kent and postdoctoral training on Class B GPCRs at the National Institute of Mental Health, he spent 15 years as a pharmacology leader at Neurocrine Biosciences, guiding in vitro biology for numerous drug discovery campaigns.
Sam is an editor at the NIH Assay Guidance Manual and regularly teaches advanced pharmacology and experimental design. His expertise in translating kinetic data from bench to bedside directly informs this Masterclass.
