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Targeting Transcriptional Enhanced Associate Domains (TEADs)
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-12-18 00:00:00 , DOI: 10.1021/acs.jmedchem.7b00879 Floriane Gibault 1 , Manon Sturbaut 1 , Fabrice Bailly 1 , Patricia Melnyk 1 , Philippe Cotelle 1, 2
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-12-18 00:00:00 , DOI: 10.1021/acs.jmedchem.7b00879 Floriane Gibault 1 , Manon Sturbaut 1 , Fabrice Bailly 1 , Patricia Melnyk 1 , Philippe Cotelle 1, 2
Affiliation
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Transcriptional enhanced associate domain (TEAD) proteins are the downstream effectors of the Hippo signaling pathway that regulate cell proliferation and stem cell functions. TEADs are unable to activate transcription and require the help of coactivators such as YAP, TAZ, VgLL, and p160 proteins. The expression of TEAD family is up-regulated in many cancer types including gastric, colorectal, breast, and prostate cancers, which is correlated with poor survival in patients. Pharmacological modulators of TEADs could therefore find application in cancer treatment and regenerative medicine. In this review, we present the very recent available structures of TEADs with or without coactivators or inhibitors and discuss the potential therapeutic application of their ligands.
中文翻译：
定位转录增强关联域（TEAD）
转录增强缔合域（TEAD）蛋白是Hippo信号通路的下游效应子，可调节细胞增殖和干细胞功能。TEAD无法激活转录，需要辅助激活剂（例如YAP，TAZ，VgLL和p160蛋白）的帮助。TEAD家族的表达在许多癌症类型中上调，包括胃癌，结肠直肠癌，乳腺癌和前列腺癌，这与患者的不良生存率相关。因此，TEADs的药理调节剂可以在癌症治疗和再生医学中找到应用。在这篇综述中，我们介绍了带有或不带有共激活剂或抑制剂的TEADs的最新可用结构，并讨论了其配体的潜在治疗应用。
更新日期：2017-12-18
中文翻译：
定位转录增强关联域（TEAD）
转录增强缔合域（TEAD）蛋白是Hippo信号通路的下游效应子，可调节细胞增殖和干细胞功能。TEAD无法激活转录，需要辅助激活剂（例如YAP，TAZ，VgLL和p160蛋白）的帮助。TEAD家族的表达在许多癌症类型中上调，包括胃癌，结肠直肠癌，乳腺癌和前列腺癌，这与患者的不良生存率相关。因此，TEADs的药理调节剂可以在癌症治疗和再生医学中找到应用。在这篇综述中，我们介绍了带有或不带有共激活剂或抑制剂的TEADs的最新可用结构，并讨论了其配体的潜在治疗应用。
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