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Profiling of GPCR complexes
Thursday, 09/16/ 2021 @ 8:00 AM - EST
- Dr. Kevin Pfleger -
- The University of Western Australia -
- Perth, Australia -
Abstract
It is highly advantageous to be able to measure GPCR ligand binding and receptor function in live cells and in real-time, and this can be achieved through biophysical detection via such technologies as bioluminescence resonance energy transfer (BRET). BRET utilizes a donor luciferase enzyme fused to a protein of interest that transfers non-radiative energy to an acceptor, such as a derivative of green fluorescent protein or a small fluorescent moiety such as BODIPY. This only occurs if donor and acceptor are within close proximity, within 10 nm of each other. We have used the BRET system to monitor ligand binding, G protein coupling, arrestin recruitment, and receptor trafficking. We have done this both with transient transfection, as well as through the luciferase-tagging of endogenous receptors using CRISPR/Cas9 gene-editing technology. We have also characterized a number of heteromer complexes using Dimerix’s Receptor Heteromer Investigation Technology. Our focus has been on inflammation, especially with respect to kidney, lung, and cardiovascular disorders, as well as cancer. We have also had a particular focus on complexes involving angiotensin and/or chemokine receptors.
About Dr. Kevin Pfleger
Professor Pfleger is Director, Biomedical Innovation at The University of Western Australia (UWA) and the MTPConnect Western Australian Life Sciences Innovation Hub. He is also Head of Molecular Endocrinology and Pharmacology at the UWA Centre for Medical Research and Harry Perkins Institute of Medical Research, Deputy Director of the Australian Research Council Centre for Personalised Therapeutics Technologies and Chief Scientific Advisor to Dimerix Limited. Professor Pfleger currently serves as President-Elect of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists and is a member of the British Pharmacological Society International Advisory Group. Professor Pfleger has developed extensive expertise in profiling receptor binding and function at the molecular and cellular levels over the last 20 years, particularly involving G protein-coupled receptors (GPCRs). He also has globally recognized expertise in bioluminescence resonance energy transfer (BRET) technology. His publications on BRET and heteromer pharmacology have been published in journals that include Nature Methods, Nature Protocols, and Nature Chemical Biology.
Author list and affiliations
- Kevin Pfleger, The University of Western Australia and Australian Research Council Centre for Personalised Therapeutics Technologies
Dr. Kevin Pfleger on the web
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