The transmembrane domains of GPCR dimers as targets for drug development

G-protein-coupled receptors (GPCRs) can form homodimers or heterodimers that modulate specific signal transduction pathways to regulate a wide range of physiological and pathological functions. As such, GPCR dimers are novel drug targets for disorders including depression, hypertension, diabetes, and vascular dementia. The interaction between two receptors in a GPCR dimer involves a conformational change in the transmembrane domain (TMD). It has been demonstrated that the TMD has an important role in GPCR dimer formation and stability in vitro and in vivo. Moreover, increasing evidence shows that the TMD of GPCRs affects the function of dimers. Therefore, the TMD of GPCRs is an emerging target for the development of drugs to treat diseases that involve GPCR dimerization.

Automated summary

GPCR dimers play important roles in regulating physiological and pathological functions, making them novel drug targets for various diseases. The formation and stability of GPCR dimers are closely associated with conformational changes in the transmembrane domain, which also affect their function. Therefore, the transmembrane domain is an emerging target for developing drugs that target GPCR dimerization.