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

Vishal Patel | Zendy; Ralph Mazitschek | Zendy; Bradley I. Coleman | Zendy; Cokey Nguyen | Zendy; Sameer Urgaonkar | Zendy; Joseph F. Cortese | Zendy; Robert H. Barker | Zendy; Edward F. Greenberg | Zendy; Weiping Tang | Zendy; James E. Bradner | Zendy; Stuart L. Schreiber | Zendy; Manoj T. Duraisingh | Zendy; Dyann F. Wirth | Zendy; Jon Clardy | Zendy

Open Access

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

Author(s) -

Vishal Patel,

Ralph Mazitschek,

Bradley I. Coleman,

Cokey Nguyen,

Sameer Urgaonkar,

Joseph F. Cortese,

Robert H. Barker,

Edward F. Greenberg,

Weiping Tang,

James E. Bradner,

Stuart L. Schreiber,

Manoj T. Duraisingh,

Dyann F. Wirth,

Jon Clardy

Publication year - 2009

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm801654y

Subject(s) - plasmodium falciparum , chemistry , histone deacetylase , small molecule , histone , acetylation , biochemistry , cell culture , microbiology and biotechnology , gene , biology , genetics , malaria , immunology

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.

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