Pin1及其小分子抑制剂的研究进展  

Recent advances in the study of Pin1 and its small-molecule inhibitors

作　　者：王淑祥[1] 李坤[1] 闻家辰[1] 刘丹[1] 赵临襄[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《中国药物化学杂志》2015年第2期135-142,共8页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(81273360)

摘　　要：Pin1(protein interaction with NIMA1)是一种肽脯氨酰顺反异构酶,其在致癌信号通路中发挥着整合、翻译和放大等重要作用。越来越多的研究表明Pin1有望成为新的肿瘤诊断和治疗的理想靶标。国内外早期对Pin1抑制剂的研究主要集中在拟肽类化合物,但由于其成药性差而难以应用于临床的先天缺陷导致近年的研究热点转移到Pin1小分子抑制剂的开发。本文综述了Pin1的生物学功能及其小分子抑制剂的最新研究进展。Pinl （protein interaction with NIMA1 ）, a kind of peptide prolyl cis-trans isomerase, plays a key role in integrating, amplifying and translating multiple oncogenic signaling pathways during oncogenesis. Studies have shown that Pinl appears to be promising target for novel anticancer therapies, and the blockade of Pinl may provide a unique way of disrupting multiple oncogenic pathways and inducing apoptosis. Early research of Pinl inhibitors were focused on peptidomimetic compounds, but recently it transfered to smallmolecule inhibitors for the defect of poor druggability and difficulty to be used in clinical of peptidomimetic compounds. In this review ,the structure and biological function of Pinl ,relationships between Pinl and oncogenesis, recent advances in the study of Pinl and its small-molecule inhibitors are summarized.

关 键 词：肽脯氨酰顺反异构酶 Pin1小分子抑制剂 肿瘤 

分 类 号：R943[医药卫生—药剂学]