A dual-mode fluorescence strategy for screening HAT modulators.

  title={A dual-mode fluorescence strategy for screening HAT modulators.},
  author={Nan Xie and Emilia N. Elangwe and Sabrina Asher and Yujun George Zheng},
  journal={Bioconjugate chemistry},
  volume={20 2},
Histone acetyltransferases (HATs) are an important class of epigenetic enzymes involved in chromatin restructuring and transcriptional regulation. We describe in this paper a novel approach for the identification and characterization of HAT inhibitors using both fluorescence resonance energy transfer (FRET) and fluorescence polarization. Expressed protein ligation (EPL) was used to label HATs PCAF and p300 with Dabcyl (Dab) as FRET acceptors. Methoxycoumarin (Mca) is conjugated to HAT substrate… CONTINUE READING