Drugs targeting the G protein-coupled receptor (GPCR) superfamily comprise 25-50% of approved small molecule therapeutics on the market today. GPCRs are universally considered to be challenging drug targets primarily due to the lack of stability of the 7 transmembrane receptor structure and the lack of information on how small molecules bind to and impact function of the receptor. However, over time, there has been some progress in understanding the structure and function of GPCRs as well as downstream signaling pathways leading to novel approaches for the discovery of the next generation of GPCR drugs. Additionally, improved pharmacological screening and validation assays have resulted in the deorphanization (identification of ligands) for several GPCRs that can be drug targets.

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Our cross-functional discovery teams have discovered and delivered several novel GPCR development candidates to our partners across multiple therapeutic areas, including inflammation, respiratory, and CNS. Regardless of the stage your GPCR project is in, partner with us to ensure you are making the right decision on your preclinical journey.

  • Precision Tuning GPCR Pathways – The Cell, Like an Engine, May Need a Tune-Up for Optimal Performance, or Even a Smooth Idle. GEN. April 2015. Full Text.