Drug Discovery

Impact of GPCR Structures on Drug Discovery

By Miles Congreve, Chris de Graaf, Nigel Swain, Christopher Tate | Apr 6, 2020


Co-founder Christopher Tate and scientists from Sosei Heptares recently published a paper in Cell which reviews the state of the art of GPCR structural biology and how it correlates with launched GPCR drugs and agents in clinical trials.


Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with over 370 structures in total bound to different ligands and the receptors in various conformational states. Structure-based drug design has been applied to an increasing number of GPCR targets over the past decade and now a few of these drug candidates have entered clinical trials. Given the length of time required for a drug to reach the market, there are no documented examples of licensed drugs being developed with the aid of a structure, but this is likely to change as current efforts come to fruition.

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