*Seminar Series: IMB Seminar Series
*Location: QBP Auditorium, Bld 80
*Date: 04/08/2017
*Time: 12.30

Speaker #1 details
*Title of talk: Structural and translational insights into GPCR allostery
*Speaker's name: Professor Arthur Christopoulos
*Speaker's organisation: Monash University
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Talk Abstract: G protein-coupled receptors (GPCRs) constitute the largest class of current drug targets, but are increasingly associated with a high attrition rate in translating fundamental preclinical discoveries into the clinic. In part, this may reflect a failure to appreciate and capture novel paradigms associated with drug action at GPCRs. Indeed, it is now well established that GPCRs possess spatially distinct and druggable allosteric sites that can be found at extracellular, transmembrane-spanning or intracellular domains. Targeting GPCR allosteric sites has the potential to lead to novel modes of GPCR subtype selectivity, signal-pathway-selective (biased) modulation and, importantly, a \"saturability\" to the allosteric effect that can be exploited to \"fine-tune\" drug responsiveness. However, many of these theoretical advantages of allosteric drugs have yet to be optimally explored in the context of disease, and this represents a significant next step for the field. Excitingly, structural biology studies are starting to identify the molecular mechanisms that underlie the pharmacological effects of allosteric modulators and are facilitating structure-based allosteric drug discovery at this important receptor family.
Speaker's bio: Arthur Christopoulos, BPharm PhD, is Professor of Pharmacology at Monash University and a Senior Principal Research Fellow of the National Health and Medical Research Council of Australia. His research focuses on novel paradigms of drug action at G protein-coupled receptors (GPCRs) and incorporates computational and mathematical modeling, medicinal chemistry, structural and chemical biology, and animal models of disease. In particular, Dr. Christopoulos\' studies focus on allosteric binding sites on GPCRs and biased agonists. He has developed assays and analytical procedures that facilitate the detection, validation and quantification of allosteric and biased drug effects, made key contributions to the discovery of first-in-class allosteric or biased ligands for muscarinic, cannabinoid, adenosine and opioid receptors, and pioneered a new mode of selective drug action involving hybrid (\"bitopic\") molecules that concomitantly bridge both orthosteric and allosteric binding sites on a single receptor. More recently, he has extended his studies towards understanding the structural basis of allosteric drug binding and modulation, as well as exploring the potential of allosteric molecules to target cognitive deficits and neuropathic pain. Dr Christopoulos has over 270 publications, over 160 invited presentations, has served on the Editorial Board of 8 journals, consults for numerous companies, and is Deputy Chair of the International Union of Clinical and Basic Pharmacology Nomenclature Committee (NC-IUPHAR). He has been a recipient of the John J. Abel Award from the American Society of Pharmacology and Experimental Therapeutics, the Rand Medal from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, the British Pharmacological Society\'s Gaddum Memorial Award, the IUPHAR James Black Analytical Pharmacology Lecturer and a Doctor of Laws (Honoris Causa) from the University of Athens. In 2014, 2015 & 2016, Thomson Reuters/Clarivate Analytics named him a Highly Cited Researcher in Pharmacology and Toxicology.

Speaker #2 details
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Other Details:
*Host name: Professor Richard Lewis
Host phone number:
*Host email: r.lewis@imb.uq.edu.au