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- W1978840260 abstract "To further evaluate elements that could contribute to the 3D topographical structure of γ-MSH, we have systematically designed a group of linear γ-MSH analogues and evaluated their biological activities: without a N-terminal acetyl, with and without a C-terminal amide, with Nle3, with l- or d-Phe6 or d-Nal(2‘)6, and with d-Trp8 or d-Nal(2‘)8. It was found that changing the C-terminal acid in γ-MSH to an amide and replacing Met with Nle leads to increased binding affinities at all four subtypes of melanocortin receptors (10−100 fold). Substitution of Trp8 with d-Nal(2‘)8 and Phe6 with d-Phe6 in γ-MSH-NH2 forms a selective antagonist for the hMC3R, whereas, substitution of Phe6 with d-Nal(2‘)6 and replacing Trp8 with d-Trp8 at γ-MSH-NH2 yields a selective partial agonist for the hMC1R. Finally, substitution of His5 with Pro5 and Trp8 with d-Nal(2‘)8 in γ-MSH-NH2 leads to a highly potent and selective agonist for the hMC1R. Molecular modeling showed that, at the C-terminal of Nle3-γ-MSH-NH2, there is a reverse-turn-like structure, suggesting that there might be a secondary binding site involved in ligand−receptor interaction for γ-MSH analogues that may explain the enhanced binding affinities of the Nle3-γ-MSH-NH2 analogues. Our results indicate that increasing the hydrophobicity and replacing Phe6 and Trp8 with bulkier aromatic amino acid residues is very important for selectivity of α-MSH/γ-MSH hybrids for hMCRs." @default.
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- W1978840260 date "2004-10-14" @default.
- W1978840260 modified "2023-09-23" @default.
- W1978840260 title "Novel 3D Pharmacophore of α-MSH/γ-MSH Hybrids Leads to Selective Human MC1R and MC3R Analogues" @default.
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- W1978840260 doi "https://doi.org/10.1021/jm049579s" @default.
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