Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors

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...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Merlino, Francesco, Zhou, Yang, Cai, Minying, Carotenuto, Alfonso, Yousif, Ali M., Brancaccio, Diego, Di Maro, Salvatore, Zappavigna, Silvia, Limatola, Antonio, Novellino, Ettore, Grieco, Paolo, Hruby, Victor J.
Formato: Artigo
Idioma:Inglês
Publicado em: 2018
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5999404/
https://ncbi.nlm.nih.gov/pubmed/29660981
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00488
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