An article Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors WOS:000501660900025 published article about PROTEIN S-PALMITOYLATION; HIPPO PATHWAY; YAP; LIGAND; CANCER; MAP in [Lu, Wenchao; Wang, Jun; Tao, Hongru; Ma, Hongna; Lu, Tian; Zhang, Dan; Ye, Xiaoqing; Ding, Hong; Yue, Liyan; Zhang, Yuanyuan; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lu, Wenchao; Li, Yong; Tang, Huanyu; Yang, Yaxi; Jiang, Hualiang; Chen, Kaixian; Zhou, Bing; Luo, Cheng] Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China; [Li, Yong; Xiong, Huan; Tang, Huanyu; Yang, Yaxi; Zhou, Bing] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Wang, Jun; Lu, Tian] Nanjing Univ Chinese Med, Jiangsu Key Lab High Technol Res TCM Formulae, 138 Xianlin Rd, Nanjing 210023, Jiangsu, Peoples R China; [Tao, Hongru] Shanghai Univ, Coll Sci, Dept Chem, 99 Shangda Rd, Shanghai 200444, Peoples R China; [Lian, Fulin; Gao, Jing; Zhang, Naixia] Chinese Acad Sci, Shanghai Inst Mat Med, Dept Analyt Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Gao, Jing] Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Ma, Hongna] Guiyang Univ Tradit Chinese Med, Dept Pharm, South Dong Qing Rd, Guiyang 550025, Guizhou, Peoples R China; [Zhang, Dan] Guizhou Univ, Sch Pharmaceut Sci, Key Lab Guizhou Fermentat Engn & Biomed, Guiyang 550025, Guizhou, Peoples R China; [Ye, Xiaoqing] Zhejiang Sci Tech Univ, Coll Life Sci, 928 2 St, Hangzhou 310018, Zhejiang, Peoples R China; [Chen, Kaixian; Luo, Cheng] Pilot Natl Lab Marine Sci & Technol Qingdao, Open Studio Druggabil Res Marine Nat Prod, 1 Wenhai Rd, Qingdao 266237, Shandong, Peoples R China; [Lu, Wenchao] Dana Farber Canc Inst, Dept Canc Biol, Boston, MA 02215 USA in 2019.0, Cited 48.0. Recommanded Product: 4-Nitrobenzoic acid. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7
Transcriptional enhancer associated domain family members (TEADs) are the most important downstream effectors that play the pivotal role in the development, regeneration and tissue homeostasis. Recent biochemical studies have demonstrated that TEAD5 could undergo autopalmitoylation that is indispensable for its function making the lipid-binding pocket an attractive target for chemical intervention. Herein, through structure-based virtual screen and rational medicinal chemistry optimization, we identified DC-TEADin02 as the most potent, selective, covalent TEAD autopalmitoylation inhibitor with the IC50 value of 197 +/- 19 nM while it showed minimal effect on TEAD-YAP interaction. Further biochemical counter-screens demonstrate the specific thiol reactivity and selectivity of DC-TEADin02 over the kinase family, lipid-binding proteins and epigenetic targets. Notably, DC-TEADin02 inhibited TEADs transcription activity leading to downregulation of YAP-related downstream gene expression. Taken together, our findings proved the validity of modulating transcriptional output in the Hippo signaling pathway through irreversible chemical interventions of TEAD5 autopalmitoylation activity, which may serve as a qualified chemical tool for TEADs palmitoylation-related studies in the future. (C) 2019 Elsevier Masson SAS. All rights reserved.
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