1.Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3.
Tian LU ; Yong LI ; Wenchao LU ; Twgm SPITTERS ; Xueyu FANG ; Jun WANG ; Simian CAI ; Jing GAO ; Yanting ZHOU ; Zhe DUAN ; Huan XIONG ; Liping LIU ; Qi LI ; Hualiang JIANG ; Kaixian CHEN ; Hu ZHOU ; Hua LIN ; Huijin FENG ; Bing ZHOU ; Christopher L ANTOS ; Cheng LUO
Acta Pharmaceutica Sinica B 2021;11(10):3206-3219
The TEA domain (TEAD) family proteins (TEAD1‒4) are essential transcription factors that control cell differentiation and organ size in the Hippo pathway. Although the sequences and structures of TEAD family proteins are highly conserved, each TEAD isoform has unique physiological and pathological functions. Therefore, the development and discovery of subtype selective inhibitors for TEAD protein will provide important chemical probes for the TEAD-related function studies in development and diseases. Here, we identified a novel TEAD1/3 covalent inhibitor (DC-TEADin1072) with biochemical IC
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