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PIN1在癌症发展中的作用及其抑制剂作为癌症治疗药物的研究

Function of PIN1 in Cancer Development and Its Inhibitors as Cancer Therapeutics.

作者信息

Yu Ji Hoon, Im Chun Young, Min Sang-Hyun

机构信息

New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Daegu, South Korea.

出版信息

Front Cell Dev Biol. 2020 Mar 17;8:120. doi: 10.3389/fcell.2020.00120. eCollection 2020.

DOI:10.3389/fcell.2020.00120
PMID:32258027
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7089927/
Abstract

Peptidyl-prolyl isomerase (PIN1) specifically binds and isomerizes the phosphorylated serine/threonine-proline (pSer/Thr-Pro) motif, which results in the alteration of protein structure, function, and stability. The altered structure and function of these phosphorylated proteins regulated by PIN1 are closely related to cancer development. PIN1 is highly expressed in human cancers and promotes cancer as well as cancer stem cells by breaking the balance of oncogenes and tumor suppressors. In this review, we discuss the roles of PIN1 in cancer and PIN1-targeted small-molecule compounds.

摘要

肽基脯氨酰异构酶（PIN1）特异性结合磷酸化的丝氨酸/苏氨酸-脯氨酸（pSer/Thr-Pro）基序并使其异构化，这会导致蛋白质结构、功能和稳定性的改变。由PIN1调节的这些磷酸化蛋白质的结构和功能改变与癌症发展密切相关。PIN1在人类癌症中高表达，并通过打破癌基因和肿瘤抑制因子的平衡来促进癌症以及癌症干细胞的发展。在本综述中，我们讨论了PIN1在癌症中的作用以及以PIN1为靶点的小分子化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd26/7089927/0165b4966bb8/fcell-08-00120-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd26/7089927/0165b4966bb8/fcell-08-00120-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd26/7089927/0165b4966bb8/fcell-08-00120-g001.jpg

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Eur J Med Chem. 2019 Sep 15;178:552-570. doi: 10.1016/j.ejmech.2019.06.018. Epub 2019 Jun 7.
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