WEBINARS


Complimentary: The new world of allosteric modulation: a dimmer switch for GPCR agonism and antagonism


GPCRs are nature’s prototypical allosteric protein and all functions of these proteins involve the transduction of ligand- induced conformational change to a third body (ie signalling protein, other ligand). There are new ligand properties that can be determined through the application of allosteric theory to GPCRs that can greatly expand knowledge and predictability of drug candidate effects. One of the main properties is probe dependence whereby GPCRs are now seen not to be mere switches but rather microprocessors that can receive different signals in and yield different signals out to the cell. In this webinar, we will cover:


lWhat is unique about designing allosteric modulators and how they modulate GPCR activity by acting as a dimmer switch. l Case studies of how Eurofins Pharma Discovery Services can be used for characterising positive and negative allosteric modulators in scales amenable to medicinal chemistry modification. lAssessing probe dependence in the form of biased agonist signalling and induced bias for PAMs and NAMs.


To register go to: http://bit.ly/2EG9NUa


A Drug Discovery WorldWebinar sponsored by:


Broadcast date: June 26, 2018


Time:


1500 GMT, 10:00 ET and 07:00 PST


Duration: 60 minutes


REGISTRATION IS FREE


Speaker


Dr Terry Kenakin Professor at the Department of Pharmacology, University of North Carolina School of Medicine


After receiving a BSc in Chemistry and PhD in Pharmacology from the University of Alberta and a post doctoral Fellowship at University College, London, Dr Kenakin worked in drug discovery at Burroughs-Wellcome (seven years) and GlaxoSmithKline (25 years) before joining the UNC School of Medicine in 2011. His work has been focused on drug receptor theory and allosteric protein function.


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