Extracellular domains and specificity of MC2R

The melanocortin type 2 receptor (MC2R or ACTHR) is the most specialized melanocortin receptor; expression in the adrenal cortex predominates, it specifically binds ACTH, and requires melanocortin receptor accessory protein 1 (MRAP) for functional activation and cell membrane localization. Fridmanis and colleagues used directed mutagenesis to investigate MC2R in detail, finding that both the ligand specificity motif and the intracellular retention signal motif are formed by a specific extracellular structure, and that an aromatic-residue-rich segment of the second extracellular loop is involved in the effects mediated by a second ACTH pharmacophore (-K-K-R-R-).

Read the full article at Fridmanis et al. (2014) Journal of Molecular Endocrinology 53 201–215. DOI:10.1530/JME-14-0169