Article
Determination of the melanocortin-4 receptor structure identifies Ca2+ as a cofactor for ligand binding.
Science (New York, N.Y.) - 24 Apr 2020
Yu Jing, Gimenez Luis E, Hernandez Ciria C, Wu Yiran, Wein Ariel H, Han Gye Won, McClary Kyle, Mittal Sanraj R, Burdsall Kylie, Stauch Benjamin, Wu Lijie, Stevens Sophia N, Peisley Alys, Williams Savannah Y, Chen Valerie, Millhauser Glenn L, Zhao Suwen, Cone Roger D, Stevens Raymond C
Abstract excerpt
The melanocortin-4 receptor (MC4R) is involved in energy homeostasis and is an important drug target for syndromic obesity. We report the structure of the antagonist SHU9119-bound human MC4R at 2.8-angstrom resolution. Ca2+ is identified as a cofactor that is complexed with residues from both the receptor and peptide ligand. Extracellular Ca2+ increases the affinity and potency of the endogenous agonist...
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