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Identification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase From Plasmodium Falciparum

Vishal Patel, Ralph Mazitschek, Bradley Coleman, Cokey Nguyen, Sameer Urgaonkar, Joseph Cortese, Robert H Barker, Edward Greenberg, Weiping Tang, James E Bradner, Stuart L Schreiber, Manoj T Duraisingh, etc.

J Med Chem. 2009 Apr 23;52(8):2185-7.

PMID: 19317450

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR42413430 HDAC 1 from Plasmodium falciparum HDAC 1 from Plasmodium falciparum Price
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