ZFIN Image: Lu et al., 2021, Fig. 2

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Figure Caption

Fig. 2 Figure 2. The discovery of DC-TEADin1072 as a covalent TEAD1 and TEAD3 autopalmitoylation inhibitor. (A) The chemical structures of DC-TEADin1072 and DC-TEADin1072-N1. (B) and (C) The inhibitory activities of DC-TEADin1072 and DC-TEADin1072-N1 in the click-based ABPP assay. The band intensity was quantified in ImageJ (NIH). The experiments were performed in biological triplicates and the data was shown as mean ± SD, n = 3. (D) DC-TEADin1072 selectively inhibited TEAD1 and TEAD3 palmitoylation while sparing TEAD2 and TEAD4. (E)‒(G) Mass spectrometry demonstrated the covalent modification of DC-TEADin1072 on TEAD1 and TEAD3 recombinant protein.

Acknowledgments

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