Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo [Asp-Pro-dPhe-Arg-Trp-Lys]- …

…, DM Smith, JA Adams, J Cheetham, M Croghan…

文献索引：Fotsch, Christopher; Smith, Duncan M.; Adams, Jeffrey A.; Cheetham, Janet; Croghan, Michael; Doherty, Elizabeth M.; Hale, Clarence; Jarosinski, Mark A.; Kelly, Michael G.; Norman, Mark H.; Tamayo, Nuria A.; Xi, Ning; Baumgartner, James W. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 14 p. 2337 - 2340

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被引用次数: 45

摘要

The solution structure of a potent melanocortin receptor agonist, Ac-Nle-cyclo [Asp-Pro-dPhe- Arg-Trp-Lys]-NH2 (1) was calculated using distance restraints determined from 1H NMR spectroscopy. Eight of the lowest energy conformations from this study were used to identify non-peptide cores that mimic the spatial arrangement of the critical tripeptide region, dPhe- Arg-Trp, found in 1. From these studies, compound 2a, containing the cis-cyclohexyl core, ...