Grieco Paolo, Carotenuto Alfonso, Campiglia Pietro, Zampelli Enrico, Patacchini Riccardo, Maggi Carlo A, Novellino Ettore, Rovero Paolo
Department of Pharmaceutical and Toxicological Chemistry, University of Naples Federico II, I-80131 Naples, Italy.
J Med Chem. 2002 Sep 26;45(20):4391-4. doi: 10.1021/jm025549i.
Replacing Cys(5) by Pen (penicillamine, beta,beta-dimethylcysteine) in the cyclic C-terminal U-II octapeptide, U-II(4-11), we have obtained a potent urotensin II (U-II) receptor agonist. Conformational analysis of solution NMR data indicated that the putative biologically active conformation of U-II is stabilized by introduction of a Pen residue. To the best of our knowledge, this is the most potent U-II receptor agonist reported to date.
在环状C末端U-II八肽U-II(4 - 11)中，用青霉胺（penicillamine，β,β - 二甲基半胱氨酸）取代半胱氨酸（Cys）(5)，我们获得了一种强效的尾加压素II（U-II）受体激动剂。溶液核磁共振数据的构象分析表明，引入一个青霉胺残基可稳定U-II假定的生物活性构象。据我们所知，这是迄今为止报道的最强效的U-II受体激动剂。
