GPCR allosterism and accessory proteins: new insights into drug discovery, 17 July 2004, Glasgow, Scotland.
This satellite meeting provided an insight into the current status and progress with GPCR allosterism and interacting accessory proteins. With one compound on the market (cinacalcet) and several others in clinical development (eg, targeting M1 and mGluR2), it is clear that targeting allosteric sites on GPCRs represents a valid approach to identifying novel drugs. Targeting allosteric sites may confer additional selectivity and permit conformational changes in GPCRs to enable disruption of large protein-protein interactions (eg, CCR5). Despite emerging research on the potential of interacting accessory proteins as drug targets, further research to understand these interactions are required before initiating focused drug discovery programs that specifically target GPCR-interacting proteins.
Organon Laboratories Ltd, Newhouse, Lanarkshire, Glasgow, ML1 5SH, UK. b.henry@organon.nhe.akzonobel.nl
Brian
B
Henry
D000494:Allosteric Regulation; D000495:Allosteric Site / Q000187:drug effects; D000818:Animals; D001688:Biological Products; D015195:Drug Design; D006801:Humans; D038622:Internationality; D008958:Models, Molecular; D011485:Protein Binding; D011487:Protein Conformation; D011956:Receptors, Cell Surface / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D012606:Scotland
D001688:Biological Products; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled