7-Transmembrane receptors

7-Transmembrane receptors (7-TM receptors), also known as G protein-coupled receptors, or GPCRs, are integral membrane proteins that contain seven membrane-spanning helices.  Many endogenous peptides activate G protein-coupled receptors.

GPCRs constitute the largest and most diverse protein family in the human genome with over 800 members identified to date.  They play critical roles in numerous cellular and physiological processes, including cell proliferation, differentiation, neurotransmission, development and apoptosis.  Aberrant receptor activity has been demonstrated in numerous disorders, and as a result GPCRs have become a very successful drug target class in pharmaceuticals treating a wide variety of indications such as pain, inflammation, neurobiological and metabolic diseases.

Further reading

Gutierrez and McDonald (2018) GPCRs: Emerging anti-cancer drug targets. Cell. Signalling 41 65 PMID: 28931490

Edin Muratspahić et al (2019) Nature-Derived Peptides: A Growing Niche for GPCR Ligand Discovery, Trends in Pharmacological Sci. 40(5) 309 PMID: 30955896

Davenport et al (2020) Advances in therapeutic peptides targeting G protein-coupled receptors. Nat. Rev. Drug Discov. 19 389 PMID: 32494050