7PIU

Cryo-EM structure of the agonist setmelanotide bound to the active melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein at 2.6 A resolution.

Summary for 7PIU

• Entry DOI: 10.2210/pdb7piu/pdb
• Related: 7PIV
• EMDB information: 13453 13454
• Descriptor: Melanocortin receptor 4, Setmelanotide (other names RM-493; BIM-22493; IRC-022493; Imcivree), Isoform Gnas-2 of Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... (8 entities in total)
• Functional Keywords: gpcr, melanocortin-4 receptor, melanocortin receptors, setmelanotide, ndp-alpha-msh, alpha-msh, antagonism, agonism, appetite regulation, anti-obesity treatment, signaling protein
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 6
• Total formula weight: 144449.67

Authors

Heyder, N.A.,Schmidt, A.,Kleinau, G.,Hilal, T.,Scheerer, P. (deposition date: 2021-08-23, release date: 2021-11-17)

• Primary citation: Heyder, N.A.,Kleinau, G.,Speck, D.,Schmidt, A.,Paisdzior, S.,Szczepek, M.,Bauer, B.,Koch, A.,Gallandi, M.,Kwiatkowski, D.,Burger, J.,Mielke, T.,Beck-Sickinger, A.G.,Hildebrand, P.W.,Spahn, C.M.T.,Hilger, D.,Schacherl, M.,Biebermann, H.,Hilal, T.,Kuhnen, P.,Kobilka, B.K.,Scheerer, P.; Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.; Cell Res., 31:1176-1189, 2021; PubMed: 34561620; DOI: 10.1038/s41422-021-00569-8

Experimental method

ELECTRON MICROSCOPY (2.58 Å)