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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|
|Date Published (YYYY/MM/DD)||2009/04/23|