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YAP, acting as a crucial transcription factor in nucleus, regulates the organ size, tissue homeostasis and tumorigenesis. Dysregulation of Hippo-YAP pathway brings a significant impact on the occurrence and development of various tumor types. Moreover, regulation of YAP/TAZ far exceeds the core kinase of the Hippo pathway, and gradually opens up new therapeutic targets. For the moment, chemotherapy together with radiotherapy act as routine methods to prolong the lives of cancer patients. Seeking more effective anti-neoplastic agents seems to be the urgent problem. This brief review focuses on the research progress of YAP inhibitors as the antineoplastic targets. Small molecule inhibitors or drugs have been discovered including verteporfin, dasatinib, statins, A35, JQ1, norcantharidin, agave, MLN8237, dobutamine and peptide-based YAP inhibitors. We are trying to seek novel therapies from the relationship between known drugs and potential mechanisms.

Citation

Zhenxue Tang, Qingxia Ma, Luyao Wang, Chaolong Liu, Hui Gao, Zhihong Yang, Zhantao Liu, Huimin Zhang, Lixia Ji, Guohui Jiang. A brief review: some compounds targeting YAP against malignancies. Future oncology (London, England). 2019 May;15(13):1535-1543

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PMID: 31066301

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