Pharmacological targeting of G protein-coupled receptor heteromers.

ABSTRACT: A main rationale for the role of G protein-coupled receptor (GPCR) heteromers as targets for drug development is the putative ability of selective ligands for specific GPCRs to change their pharmacological properties upon GPCR heteromerization. The present study provides a proof of concept for this rationale by demonstrating that heteromerization of dopamine D₁ and D₃ receptors (D₁R and D₃R) influences the pharmacological properties of three structurally similar selective dopamine D₃R ligands, the phenylpiperazine derivatives PG01042, PG01037 and VK4-116. By using D₁R-D₃R heteromer-disrupting peptides, it could be demonstrated that the three D₃R ligands display different D₁R-D₃R he

SUBMITTER: Moreno E 

PROVIDER: S-EPMC9645299 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature