6fce

NMR ensemble of Macrocyclic Peptidomimetic Containing Constrained a,a-dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors

spinqualitylabelsall models 6fce Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6fce is a 1 chain structure with sequence from Synthetic construct. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Solution NMR, 10 models Ligands: AC5, DPN, NH2 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed We report the development of macrocyclic melanocortin derivatives of MT-II and SHU-9119, achieved by modifying the cycle dimension, and incorporating constrained amino acids in ring-closing. This study culminated in the discovery of novel agonists/antagonists with an unprecedented activity profile, by adding pieces to the puzzle of the melanocortin receptor selec-tivity. Finally, the resulting 19- and 20-membered rings represent a suitable frame for the design of further therapeutic ligands as selective modulators of the melanocortin system. Development of Macrocyclic Peptidomimetics Containing Constrained alpha,alpha-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.,Merlino F, Zhou Y, Cai M, Carotenuto A, Yousif AM, Brancaccio D, Di Maro S, Zappavigna S, Limatola A, Novellino E, Grieco P, Hruby VJ J Med Chem. 2018 Apr 16. doi: 10.1021/acs.jmedchem.8b00488. PMID:29660981 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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