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.