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Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
| Publication Type | Journal Article |
| Authors | Patel, V., Mazitschek R., Coleman B., Nguyen C., Urgaonkar S., Cortese J., Barker RH, Greenberg E., Tang W., Bradner JE, Schreiber SL, Duraisingh MT, Wirth DF, and Clardy J. |
| Abstract | 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 established. |
| Year of Publication | 2009 |
| Journal | Journal of medicinal chemistry |
| Volume | 52 |
| Issue | 8 |
| Pages | 2185-7 |
| Date Published (YYYY/MM/DD) | 2009/04/23 |
| ISSN Number | 0022-2623 |
| DOI | 10.1021/jm801654y |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/19317450?dopt=Abstract |
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