|Publication Type||Journal Article|
|Year of Publication||2009|
|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, Clardy, J|
|Journal||Journal of medicinal chemistry|
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.