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A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities

文献类型：期刊论文

作者Lou, Jianfeng4,5,6; Lu, Yuhang4,5,6; Cheng, Jing4,5,6; Zhou, Feilong5,6; Yan, Ziqin5,6; Zhang, Daizhou3; Meng, Xiangjing3; Zhao, Yujun1,2,3,4,5,6
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2022-12-05
卷号243页码:31
ISSN号0223-5234
关键词TEAD YAP Palmitoylation Protein-protein interaction Covalent inhibitor
DOI10.1016/j.ejmech.2022.114684
通讯作者Meng, Xiangjing(fredamxj@163.com) ; Zhao, Yujun(yjzhao@simm.ac.cn)
英文摘要TEADs are transcription factors and core downstream components of the Hippo pathway. Mutations of the Hippo pathway and/or dysregulation of YAP/TAZ culminate in aberrant transcriptional activities of TEADs, which were considered as key contributing factors of mesotheliomas, fibrotic diseases, Alzheimer's diseases, Huntington's diseases, suppressive immune response, and drug resistance, among others. To modulate transcriptional activities of TEADs, several pharmacological approaches have been pursued, including TEAD/YAP protein-protein inter-action inhibitors, TEAD PBP inhibitors, and TEAD activators. As summarized in this review, a large number of inhibitors and activators of TEADs have been reported with decent in vitro potencies, a few exerted robust and compelling in vivo efficacies, and three that are undergoing clinical trials for the treatment of human cancers. Despite clinical advancement of the TEAD PBP inhibitors, development of other types TEAD inhibitors and ac-tivators generally lags behind. Information showcased herein might benefit discovery of next generation TEAD modulators for treatment of human oncological diseases and beyond.
WOS关键词PROTEIN-PROTEIN INTERACTION ; SMALL-MOLECULE INHIBITORS ; YES-ASSOCIATED PROTEIN ; ORGAN SIZE CONTROL ; TUMOR-SUPPRESSOR ; HIPPO PATHWAY ; PROMOTES RESISTANCE ; TISSUE HOMEOSTASIS ; CELL-PROLIFERATION ; SIGNALING PATHWAY
资助项目National Natural Science Foundation of China[82073682] ; National Natural Science Foundation of China[81872724] ; Jinan Innovation Team Project[2021GXRC069] ; Science and Technology Commission of Shanghai Municipality[22ZR1474500] ; Science and Technology Commission of Shanghai Municipality[18431907100]
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号WOS:000874958900003
源URL[http://119.78.100.183/handle/2S10ELR8/303145]  
专题新药研究国家重点实验室
通讯作者Meng, Xiangjing; Zhao, Yujun
作者单位1.Zhengzhou Univ, Key Lab Adv Drug Preparat Technol, Minist Educ, Zhengzhou 450001, Peoples R China
2.Zhengzhou Univ, Sch Pharmaceut Sci, Minist Educ, Zhengzhou 450001, Peoples R China
3.Shandong Acad Pharmaceut Sci, Shandong Prov Key Lab Biopharmaceut, Jinan 250101, Peoples R China
4.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, Small Mol Drug Res Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
6.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Lou, Jianfeng,Lu, Yuhang,Cheng, Jing,et al. A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2022,243:31.
APA Lou, Jianfeng.,Lu, Yuhang.,Cheng, Jing.,Zhou, Feilong.,Yan, Ziqin.,...&Zhao, Yujun.(2022).A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,243,31.
MLA Lou, Jianfeng,et al."A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 243(2022):31.

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来源：上海药物研究所

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