Pin1及其抑制剂的研究进展  

Recent advances in the study of Pin1 and its inhibitors

作　　者：张崇敬[1] 张志辉[2] 徐柏玲[1] 王玉玲[2] 

机构地区：[1]中国医学科学院、中国协和医科大学药物研究所,北京100050 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《药学学报》2008年第1期9-17,共9页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金青年科学基金资助项目(30500634).

摘　　要：Pin1是一个新的肽脯氨酰异构酶,特异性地催化蛋白质中磷酸化的Ser/Thr-Pro酰胺键的顺反异构,改变蛋白质的构象,调控蛋白质的功能。抑制Pin1的表达和活性,可抑制肿瘤细胞的生长。Pin1抑制剂有望发展成为新作用机制的抗癌药物。本文综述了近年来Pin1及其抑制剂研究的最新进展。Pinl is a phosphorylation-dependent peptidyl-prolyl cis/trans isomerase, which specifically catalyzes the amide bond isomerization of phosphoserine-proline or phosphothreonine-proline in mitotic phosphoproteins. Pinl induces the conformational changes to control the function of phosphoproteins. Depletion of Pinl on various human cancer cell lines cause mitotic arrest and apoptosis. Pinl is an attracting therapeutic target for anticancer and its inhibitors might be potential anticancer drug. In this review, Pinl inhibitors and the catalytic mechanism, the biological function of Pinl and its role in oncogenesis are summarized.

关 键 词：肽脯氨酰异构酶 Pin1抑制剂 肿瘤 综述 

分 类 号：R916[医药卫生—药学]