You are here

Journal of medicinal chemistry DOI:10.1021/jm801654y

Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.

Publication TypeJournal Article
Year of Publication2009
AuthorsPatel, 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
JournalJournal of medicinal chemistry
Volume52
Issue8
Pages2185-7
Date Published2009/04/23
ISSN0022-2623
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.

URLhttp://dx.doi.org/10.1021/jm801654y
DOI10.1021/jm801654y
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/19317450?dopt=Abstract