脯氨酰内肽酶(prolyl endopeptidase,PEP)[EC3.4.21.26]是一种能特异性水解多肽链中脯氨酸残基羧基端肽键的丝氨酸蛋白酶,能降解许多多肽类神经递质和激素,其活性的异常会引起精神、认知过程的障碍.一些PEP的专一性抑制剂(如JTP-4819)显示在莨菪胺引起的小鼠记忆障碍模型中有改善记忆的药理作用.猪肌肉PEP晶体结构的解析推动了PEP的研究.
Prolyl endopeptidase(PEP) [EC 3.4.21.26] is a new class of serine protease, which is capable of hydrolyzing a substrate on the carboxyl site of proline residue located internally in a peptide. It can hydrolyse several peptide hormones and neuotransmitters, so abnormal raise and decrease of PEP activity would result in diseases related to memory and cognition. Specific inhibitor for example JTP-4819 shows a good pharmaceutical effect in reversing scopolamine-induced amnesia in rats. The analysis of crystral structure of PEP from porcine muscle has greatly promoted the research on PEP.
李民,陈常庆.脯氨酰内肽酶研究进展[J].生物化学与生物物理进展,2000,27(2):171-174
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