Wilson K R, Todorovic A, Proneth B, Haskell-Luevano C
Department of Medicinal Chemistry, University of Florida, 1600 SW Archer Road PO Box 100485, Gainesville, FL 32610, USA.
Cell Mol Biol (Noisy-le-grand). 2006 May 30;52(2):3-20.
The melanocortin system consists of five seven-transmembrane spanning G-protein coupled (GPCRs) receptors (MC1R-MC5R), the endogenous agonists a-, B- and melanocyte stimulating hormone (MSH), adrenocorticotropic hormone (ACTH), and the endogenous antagonists Agouti and Agouti-related protein (AGRP). Melanocortin agonists are involved in the regulation of feeding behavior and weight omeostasis in mammals. Structure-activity relationships (SAR) have been performed on the endogenous melanocortin receptor agonists and antagonists that have identified ligand amino acid residues implicated as important for receptor binding and stimulation. Knowledge of putative ligand-receptor interactions may help to design molecules as therapeutic agents for the treatment of physiological diseases.
黑皮质素系统由五个七跨膜的G蛋白偶联受体（GPCRs）（MC1R - MC5R）、内源性激动剂α-、β-和促黑素细胞激素（MSH）、促肾上腺皮质激素（ACTH）以及内源性拮抗剂刺鼠信号蛋白和刺鼠相关蛋白（AGRP）组成。黑皮质素激动剂参与哺乳动物进食行为和体重稳态的调节。已经对内源性黑皮质素受体激动剂和拮抗剂进行了构效关系（SAR）研究，确定了对受体结合和刺激起重要作用的配体氨基酸残基。对假定的配体-受体相互作用的了解可能有助于设计分子作为治疗生理疾病的治疗剂。
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