Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides
Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His 6 with phenyl-containing rigid templates in achieving good hMC4R agonist potency and selectivity against hMC1R in linear pentapeptides.
Chu, Xin-Jie,Bartkovitz, David,Danho, Waleed,Swistok, Joseph,Cheung, Adrian Wai-Hing,Kurylko, Grazyna,Rowan, Karen,Yeon, Mitch,Franco, Lucia,Qi, Lida,Chen, Li,Yagaloff, Keith
p. 4910 - 4914
(2007/10/03)
Selective cyclic peptides with melanocortin-4 receptor (MC4-R) agonist activity
Peptides cyclized via disulfide or lactam bridges having melanocortin-4 receptor (MC4-R) agonist activity useful for treatment of obesity.
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(2008/06/13)
Selective linear peptides with melanocortin-4 receptor (MC4-R) agonist activity
Peptides of formulae I, II and III selectively activate melanocortin-4 (MC-4) receptor activity.
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(2008/06/13)
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