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

dc.contributor.authorNguyen, Cokey
dc.contributor.authorUrgaonkar, Sameer
dc.contributor.authorCortese, Joseph
dc.contributor.authorBarker, Robert H.
dc.contributor.authorGreenberg, Edward
dc.contributor.authorTang, Weiping
dc.contributor.authorPatel, Vishal
dc.contributor.authorMazitschek, Ralph
dc.contributor.authorColeman, Bradley Ian
dc.contributor.authorBradner, James Elliott
dc.contributor.authorSchreiber, Stuart L.
dc.contributor.authorDuraisingh, Manoj T.
dc.contributor.authorWirth, Dyann Fergus
dc.contributor.authorClardy, Jon C.
dc.date.accessioned2010-10-07T17:17:45Z
dc.date.issued2009
dc.identifier.citationPatel, 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.issn0022-2623en_US
dc.identifier.urihttp://nrs.harvard.edu/urn-3:HUL.InstRepos:4461121
dc.description.abstractA 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.sponsorshipChemistry and Chemical Biologyen_US
dc.language.isoen_USen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.isversionofdoi:10.1021/jm801654yen_US
dc.relation.hasversionhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC2669731/pdf/en_US
dash.licenseOAP
dc.titleIdentification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase from Plasmodium falciparumen_US
dc.typeJournal Articleen_US
dc.description.versionVersion of Recorden_US
dc.relation.journalJournal of Medicinal Chemistryen_US
dash.depositing.authorSchreiber, Stuart L.
dc.date.available2010-10-07T17:17:45Z
dc.identifier.doi10.1021/jm801654y*
dash.authorsorderedfalse
dash.contributor.affiliatedColeman, Bradley
dash.contributor.affiliatedPatel, Vishal
dash.contributor.affiliatedDuraisingh, Manoj
dash.contributor.affiliatedWirth, Dyann
dash.contributor.affiliatedBradner, James E
dash.contributor.affiliatedSchreiber, Stuart
dash.contributor.affiliatedClardy, Jon
dash.contributor.affiliatedMazitschek, Ralph


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