IMB Seminar Series - Professor Arthur Christopoulos 'Structural and translational insights into GPCR allostery'
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- 'Structural and translational insights into GPCR allostery' - Arthur Christopoulos
Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences,
Monash University, Australia
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.
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