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. 2021 Aug 27;31(10):1061–1071. doi: 10.1038/s41422-021-00557-y

Fig. 4. Structural basis of differential activities among melanocortin peptide ligands.

Fig. 4

a, b Structural comparison of α-MSH-bound MC1R complex (a, b), afamelanotide-bound MC1R complex (a), SHU9119-bound MC1R complex (b) and SHU9119-bound MC4R complex (PDB: 6W25; a, b). The conformational changes of W2546.48, F2576.51, and F2807.35 upon MC1R activation are emphasized. The alignment was based on the receptors and MC1R residue numbers are colored in medium purple. c Comparison of SHU9119-binding pocket in MC1R and MC4R. M1283.36 of MC1R forms steric clash with D-NalU7 and W2546.48, making SHU9119 a partial agonist for MC1R. Hydrogen bonds are shown as red dash lines.