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Preparation and Delivery of Protein Microcrystals in Lipidic Cubic Phase for Serial Femtosecond Crystallography
Published on: September 20, 2016
Opioid and chemokine receptor heterodimers: arranged marriages or dangerous liaisons?
1Department of Pharmacology and Therapeutics, Faculty of Medicine, 13th floor, Room 1303, McIntyre Medical Sciences Building, 3655 Promenade Sir William Osler, Montreal, QC, Canada, H3G 1Y6. terence.hebert@mcgill.ca
Abstract:
Heterodimerization of GPCRs (G-protein-coupled receptors) has begun to be appreciated as a rich new vein for drug discovery. The possibility of developing modulators for different GPCRs which work at allosteric sites other than the ligand-binding site is not new, but the notion of using a dimeric receptor partner as the target for this intervention has not yet percolated into the broader industrial community. In the present article, I discuss this notion in the context of the heterodimeric delta-opioid receptor-CXCR2 chemokine receptor dimer identified by Parenty et al., in this issue of the Biochemical Journal.
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