[Pin1及其抑制剂的研究新进展]
[Recent advances in the study of pin1 and its inhibitors].
作者信息
Zhang Chong-Jing, Zhang Zhi-Hui, Xu Bai-Ling, Wang Yu-Ling
机构信息
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
出版信息
Yao Xue Xue Bao. 2008 Jan;43(1):9-17.
Pin1 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. Pin1 induces the conformational changes to control the function of phosphoproteins. Depletion of Pinl on various human cancer cell lines cause mitotic arrest and apoptosis. Pin1 is an attracting therapeutic target for anticancer and its inhibitors might be potential anticancer drug. In this review, Pin1 inhibitors and the catalytic mechanism, the biological function of Pin1 and its role in oncogenesis are summarized.
Pin1是一种磷酸化依赖性肽基脯氨酰顺/反异构酶，它特异性催化有丝分裂磷酸化蛋白中磷酸丝氨酸-脯氨酸或磷酸苏氨酸-脯氨酸的酰胺键异构化。Pin1诱导构象变化以控制磷酸化蛋白的功能。在各种人类癌细胞系中敲低Pin1会导致有丝分裂停滞和凋亡。Pin1是一个有吸引力的抗癌治疗靶点，其抑制剂可能是潜在的抗癌药物。在这篇综述中，总结了Pin1抑制剂及其催化机制、Pin1的生物学功能及其在肿瘤发生中的作用。
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