Dr. GPCR Ecosystem
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Quantifying the kinetics of GPCR signaling
Abstract
Recently there has been an explosion of interest in measuring the kinetics of GPCR signaling, enabled by biosensor technology. Curve fitting, the foundation of quantitative pharmacology, is rarely applied to time-course data. Sam will demonstrate straightforward curve fitting techniques for kinetic GPCR data, using GraphPad Prism, and show the insights obtained from the results. Examples include mu opioid partial agonism and bias quantified using Montana Molecular biosensors, arrestin mechanism analysis, illicit synthetic cannabinoid efficacy quantification, and G-protein selectivity of the GIP receptor.
Thank you to Dr. Shivani Sachdev for the cannabinoid receptor data she generated in Mark Connor’s lab and Matthew Harris for the data he acquired in Graham Ladd’s lab using the GIP receptor.
Original data can be found in the publications below :
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In vitro determination of the efficacy of illicit synthetic cannabinoids at CB1 receptors
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RAMPs regulate signaling bias and internalization of the GIPR
About Dr. Samuel Hoare
Dr. Hoare is a pharmacology data analyst and the founder of Pharmechanics LLC. As an industry pharmacologist, he consults with numerous pharma and biotechs in understanding and applying in vitro pharmacology data to advance drug discovery. He specializes in kinetic analysis of drug action and is known for applying binding kinetics to the development of effective therapeutics, particularly GPCR antagonists.
Sam completed his Ph.D. in biochemistry, studying allosteric modulation of dopamine receptors, from the University of Kent, United Kingdom. He then moved to the National Institute of Mental Health, researching pharmacological mechanisms of Class B GPCRs as part of his postdoctoral training.
Dr. Hoare worked as a pharmacology leader in the pharmaceutical industry for 15 years at Neurocrine Biosciences. He guided the in vitro biology efforts of the company for numerous drug discovery campaigns.
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