Impact of GPCR Structures on Drug Discovery

Cell. 2020 Apr 2;181(1):81-91. doi: 10.1016/j.cell.2020.03.003.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Drug Design*
  • Drug Discovery*
  • Humans
  • Ligands
  • Molecular Conformation
  • Molecular Structure
  • Receptors, G-Protein-Coupled / chemistry*


  • Ligands
  • Receptors, G-Protein-Coupled