摘要
肽基脯氨酰顺/反异构酶Pin1,是一种由酵母ESS1的人类直系同源物与来自各种蛋白质中的多肽pSer/pThr-Pro残基特异性异构结合产生的,能调节磷酸化蛋白的表达水平和功能的异构酶。Pin1的活化与多种疾病的病理机制相关,如癌症、阿尔茨海默氏病、感染性疾病等。因此,调节能够调节Pin1的化合物可以作为治疗这些疾病的临床药物。许多化学家们已经致力于合成基于Pin1的三维结构的抑制剂。我们已经从天然产物包括功能性食品和功能性食品中筛选了Pin1的抑制剂。在这里,我们综述了Pin1相关的病理机制和已知的从天然产物中确定的从天然产物中确定的已知抑制剂,并引入了针对Pin1活性的筛选方法。
关键词: 抑制剂,天然产物,Pin1,筛选。
Current Drug Targets
Title:Role of Prolyl Isomerase Pin1 in Pathogenesis of Diseases and Remedy for the Diseases from Natural Products
Volume: 15 Issue: 10
Author(s): Katsuhiko Takahashi, Taiki Shimizu, Keita Kosaka, Masafumi Hidaka, Chiyoko Uchida and Takafumi Uchida
Affiliation:
关键词: 抑制剂,天然产物,Pin1,筛选。
摘要: The peptidyl prolyl cis/trans isomerase Pin1, the human ortholog of yeast Ess1 specifically isomerizes peptide bindings of pSer/pThr-Pro residues in various proteins, and regulates the expression levels and functions of phosphorylated proteins. Activation of Pin1 is associated with pathology of a variety of diseases, such as cancer, Alzheimer’s disease, infectious diseases and so on. Therefore, regulatory compounds for Pin1 can be applied as a clinical medicine against these diseases. Many chemists have exerted themselves to synthesize the inhibitors based on the 3D structure of Pin1. We have screened for the inhibitors against Pin1 from the natural products including the functional foods. Here we review the Pin1-associated pathology and the known inhibitors identified from natural products. And we introduce the screening methods targeting Pin1 activity.
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Cite this article as:
Takahashi Katsuhiko, Shimizu Taiki, Kosaka Keita, Hidaka Masafumi, Uchida Chiyoko and Uchida Takafumi, Role of Prolyl Isomerase Pin1 in Pathogenesis of Diseases and Remedy for the Diseases from Natural Products, Current Drug Targets 2014; 15 (10) . https://dx.doi.org/10.2174/1389450115666140903110724
DOI https://dx.doi.org/10.2174/1389450115666140903110724 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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