Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60.

@article{Wu2009BisubstrateIO,
  title={Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60.},
  author={Jiang X. Wu and Nan Xie and Zhikun Wu and Ying Fang Zhang and Yujun George Zheng},
  journal={Bioorganic & medicinal chemistry},
  year={2009},
  volume={17 3},
  pages={1381-6}
}
Esa1 (essential Sas2-related acetyltransferase 1) and Tip60 (HIV-1 TAT-interactive protein, 60 kDa) are key members of the MYST family of histone acetyltransferases (HATs) and play important functions in many cellular processes. In this work, we designed, synthesized and evaluated a series of substrate-based analogs for the inhibition of Esa1 and Tip60. The structures of these analogs feature that coenzyme A is covalently linked to the side chain amino group of the acetyl lysine residues in the… CONTINUE READING

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