一种新的、强效的尾加压素II受体肽激动剂，其在二硫键处含有一个Pen残基。
A new, potent urotensin II receptor peptide agonist containing a Pen residue at the disulfide bridge.
作者信息
Grieco Paolo, Carotenuto Alfonso, Campiglia Pietro, Zampelli Enrico, Patacchini Riccardo, Maggi Carlo A, Novellino Ettore, Rovero Paolo
机构信息
Department of Pharmaceutical and Toxicological Chemistry, University of Naples Federico II, I-80131 Naples, Italy.
出版信息
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。
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