'Reverse Pharmacology' Approach To GPCR-Focused Drug Discovery
Monday, March 18, 2013 - 10:21
in Physics & Chemistry
A new paper in Molecular Pharmacology describes how 'reverse pharmacology', enabled by Heptares Therapeutics StaR(R) technology, can be applied to and accelerate GPCR-based drug discovery. The paper utilized the study of isolated GPCRs locked in conformations that correspond to agonist or antagonist pharmacology, and the elucidation of their respective 3D structures. These StaRs and structures can be used to select and design compounds with specific pharmacologies, such as inverse agonist, partial agonist or full agonist, based on their ability to bind differentially to the agonist and antagonist StaRs. For example a full agonist will preferentially bind to the agonist StaR. read more