Article
Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling.
Science (New York, N.Y.) - 21 May 2021
Israeli Hadar, Degtjarik Oksana, Fierro Fabrizio, Chunilal Vidicha, Gill Amandeep Kaur, Roth Nicolas J, Botta Joaquin, Prabahar Vadivel, Peleg Yoav, Chan Li F, Ben-Zvi Danny, McCormick Peter J, Niv Masha Y, Shalev-Benami Moran
Abstract excerpt
Obesity is a global epidemic that causes morbidity and impaired quality of life. The melanocortin receptor 4 (MC4R) is at the crux of appetite, energy homeostasis, and body-weight control in the central nervous system and is a prime target for anti-obesity drugs. Here, we present the cryo-electron microscopy (cryo-EM) structure of the human MC4R-Gs signaling complex bound to the agonist setmelanotide, a cyclic...
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