Identification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase from Plasmodium falciparum

@inproceedings{Patel2009IdentificationAC,
  title={Identification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase from Plasmodium falciparum},
  author={Vishal K. Patel and Ralph Mazitschek and Bradley Coleman and Cokey Nguyen and Sameer Urgaonkar and Joseph F. Cortese and Robert H. Barker and Edward Greenberg and Weiping Tang and James E. Bradner and Stuart L. Schreiber and Manoj Duraisingh and Dyann F Wirth and Jon Clardy},
  booktitle={Journal of medicinal chemistry},
  year={2009}
}
A library of approximately 2000 small molecules biased toward inhibition of histone deacetylases was assayed for antimalarial activity in a high-throughput P. falciparum viability assay. Active compounds were cross-analyzed for induction of histone hyperacetylation in a human myeloma cell line to identify HDAC inhibitors with selectivity for P. falciparum over the human host. To verify on-target selectivity, pfHDAC-1 was expressed and purified and a biochemical assay for pfHDAC-1 activity was… CONTINUE READING
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