Event Details

Friday, 04 August 2017
12:30 pm - 1:00 pm
Queensland Bioscience Precinct Auditorium - Building 80, The University of Queensland
UQ Location:
Queensland Bioscience Precinct (St Lucia)
Event category(s):

Event Contact

Ms Katrina Garner-Moore
3366 2110
Org. Unit:
Institute for Molecular Bioscience

Event Description

Full Description:
'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.

Directions to UQ

Google Map:
To St Lucia Campus, UQ Ipswich, and UQ Gatton.

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