Signal Transduction and Pathogenic Modifications at the Melanocortin-4 Receptor: A Structural Perspective.

ABSTRACT: The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast, the agouti-related peptide (AgRP) acts as an endogenous inverse agonist and suppresses ligand-independent basal signaling activity (orexigenic effects). Binding of ligands to MC4R leads to the activation of different G-protein subtypes or arrestin and concomitant signaling pathways. This receptor is a key protein in the hypothalamic regulation of food intake and energy expenditure and naturally-occurring inactivating MC4R variants are the most frequent cause of monogenic obesity. In general, obesity is a growing problem on a global scale and is of social, medical, and economic relevance. A significant goal is to devel

SUBMITTER: Heyder N 

PROVIDER: S-EPMC6685040 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature