YAP,作为细胞核中的关键转录因子,调节器官的大小,组织稳态和肿瘤发生。Hippo-YAP通路的失调对多种肿瘤的发生、发展产生重要影响。此外,YAP/TAZ的调节远远超过Hippo途径的核心激酶,并逐步开拓新的治疗靶点。目前,化疗和放疗是延长癌症患者生命的常规方法。寻求更有效的抗肿瘤药物似乎是当务之急。本文就YAP抑制剂作为抗肿瘤靶点的研究进展作一综述。已经发现了小分子抑制剂或药物,包括维替泊芬,达沙替尼,他汀类药物,A35,JQ1,去甲斑三酮,龙舌兰,MLN8237、多巴酚丁胺和基于肽的YAP抑制剂。我们正试图从已知药物和潜在机制之间的关系中寻求新的治疗方法。
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.