Rules of Engagement: GPCRs and G Proteins
Alisa Glukhova, Christopher J Draper-Joyce, Roger K Sunahara, Arthur Christopoulos, Denise Wootten, Patrick M Sexton
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE | AMER CHEMICAL SOC | Published : 2018
G protein-coupled receptors (GPCRs) are a key drug target class. They account for over one-third of current pharmaceuticals, and both drugs that inhibit and promote receptor function are important therapeutically; in some cases, the same GPCR can be targeted with agonists and inhibitors, depending upon disease context. There have been major breakthroughs in understanding GPCR structure and drug binding through advances in X-ray crystallography, and membrane protein stabilization. Nonetheless, these structures have predominately been of inactive receptors bound to inhibitors. Efforts to capture structures of fully active GPCRs, in particular those in complex with the canonical, physiological ..View full abstract
P.M.S. is a Principal Research Fellow of the National Health and Medical Research Council of Australia (NHMRC). A.C. is a Senior Principal Research Fellow of the NHMRC. D.W. is a Career Development Fellow of the NHMRC. A.G. is an Australian Research Council (ARC) Discovery Early Career Researcher Award recipient.