Bisubstrate analogue structure-activity relationships for p300 histone acetyltransferase inhibitors.

@article{Sagar2004BisubstrateAS,
  title={Bisubstrate analogue structure-activity relationships for p300 histone acetyltransferase inhibitors.},
  author={Vatsala Sagar and Weiping Zheng and Paul M. Thompson and Philip A Cole},
  journal={Bioorganic & medicinal chemistry},
  year={2004},
  volume={12 12},
  pages={3383-90}
}
p300 and CBP are important histone acetyltransferases (HATs) that regulate gene expression and may be anti-cancer drug targets. Based on a previous lead compound, Lys-CoA, we have used solid phase synthesis to generate a series of 11 new analogues and evaluated these compounds as HAT inhibitors. Increased spacing between the CoA moiety and the lysyl moiety… CONTINUE READING