The Role of Lipids in Allosteric Modulation of Dopamine D₂ Receptor-In Silico Study.

ABSTRACT: The dopamine D₂ receptor, belonging to the class A G protein-coupled receptors (GPCRs), is an important drug target for several diseases, including schizophrenia and Parkinson's disease. The D₂ receptor can be activated by the natural neurotransmitter dopamine or by synthetic ligands, which in both cases leads to the receptor coupling with a G protein. In addition to receptor modulation by orthosteric or allosteric ligands, it has been shown that lipids may affect the behaviour of membrane proteins. We constructed a model of a D₂ receptor with a long intracellular loop (ICL3) coupled with G_iα1 or G_iα2 proteins, embedded in a complex asymmetric membrane, and simulated it in complex with positive, negative or neutral allosteric ligands.

SUBMITTER: Zuk J 

PROVIDER: S-EPMC8874991 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature