摘要
Hippo信号通路对于调节组织稳态、器官大小和肿瘤发生中是至关重要的。YAP和TAZ,Hippo信号通路的两个主要效应蛋白,是转录共激活因子并主要通过与TEAD家族转录因子的相互作用促进靶基因的表达。作为癌基因蛋白,YAP和TAZ在各种癌症样本中被频繁激活或高表达。此外,它们的活动被认为与几种广泛使用的抗癌药物的耐药有关,且YAP活化有助于肿瘤的复发。因此,Hippo通路,特别是YAP/TAZ-TEAD相互作用,是抗癌治疗的一个引人注目的靶点。本文将讨论抑制Yap / TAZ活性的可能途径,并综述目前可用的靶向Hippo通路的小分子。
关键词: Hippo,TAZ, TEAD,Verteporfin,VGLL4, YAP。
Current Medicinal Chemistry
Title:Targeting the Hippo Pathway for Anti-cancer Therapies
Volume: 22 Issue: 35
关键词: Hippo,TAZ, TEAD,Verteporfin,VGLL4, YAP。
摘要: The Hippo signaling pathway is critical in regulating tissue homeostasis, organ size, and tumorigenesis. YAP and TAZ, two major effectors of the Hippo pathway, function as transcriptional co-activators and promote target gene expression mainly through interaction with TEAD family transcription factors. As oncoproteins, YAP and TAZ are frequently activated or highly expressed in various cancer specimens. Moreover, their activity has been linked to resistance to a few widely used anti-cancer drugs, and YAP activation contributes to cancer relapse. Thus, the Hippo pathway, especially YAP/TAZ-TEAD interaction, represents an attractive target for anti-cancer therapies. Here, we will discuss potential approaches to inhibit YAP/TAZ activity, and also review currently available small molecules targeting the Hippo pathway.
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Targeting the Hippo Pathway for Anti-cancer Therapies, Current Medicinal Chemistry 2015; 22 (35) . https://dx.doi.org/10.2174/0929867322666151002112256
DOI https://dx.doi.org/10.2174/0929867322666151002112256 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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