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

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

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dc.contributor.author Nguyen, Cokey
dc.contributor.author Urgaonkar, Sameer
dc.contributor.author Cortese, Joseph
dc.contributor.author Barker, Robert H.
dc.contributor.author Greenberg, Edward
dc.contributor.author Tang, Weiping
dc.contributor.author Patel, Vishal
dc.contributor.author Mazitschek, Ralph
dc.contributor.author Coleman, Bradley Ian
dc.contributor.author Bradner, James Elliott
dc.contributor.author Schreiber, Stuart L.
dc.contributor.author Duraisingh, Manoj T.
dc.contributor.author Wirth, Dyann Fergus
dc.contributor.author Clardy, Jon C.
dc.date.accessioned 2010-10-07T17:17:45Z
dc.date.issued 2009
dc.identifier.citation Patel, Vishal, Ralph Mazitschek, Bradley Coleman, Cokey Nguyen, Sameer Urgaonkar, Joseph Cortese, Robert H. Barker, et al. 2009. Identification and characterization of small molecule inhibitors of class I Histone deacetylase from Plasmodium falciparum. Journal of Medicinal Chemistry 52:2185-2187. en_US
dc.identifier.issn 0022-2623 en_US
dc.identifier.uri http://nrs.harvard.edu/urn-3:HUL.InstRepos:4461121
dc.description.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. en_US
dc.description.sponsorship Chemistry and Chemical Biology en_US
dc.language.iso en_US en_US
dc.publisher American Chemical Society en_US
dc.relation.isversionof doi:10.1021/jm801654y en_US
dc.relation.hasversion http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2669731/pdf/ en_US
dash.license OAP
dc.title Identification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase from Plasmodium falciparum en_US
dc.type Journal Article en_US
dc.description.version Version of Record en_US
dc.relation.journal Journal of Medicinal Chemistry en_US
dash.depositing.author Schreiber, Stuart L.
dc.date.available 2010-10-07T17:17:45Z

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  • FAS Scholarly Articles [7594]
    Peer reviewed scholarly articles from the Faculty of Arts and Sciences of Harvard University

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