Agouti-related protein functions as an inverse agonist at a constitutively active brain melanocortin-4 receptor

C Haskell-Luevano, EK Monck - Regulatory peptides, 2001 - Elsevier
Agouti-related protein (AGRP) is one of two naturally occurring antagonists of G-Protein
coupled receptors (GPCRs) identified to date, and has been physiologically implicated in
regulating food intake, body weight, and energy homeostasis. AGRP has been identified in
vitro, as competitively antagonizing the brain melanocortin-4 (MC4R) and melanocortin-3
(MC3R) receptors, and when over expressed in transgenic mice, results in an obese
phenotype. Emerging data propose that AGRP has additional targets in the hypothalamus …