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
| Title: | Identification and Characterization of Small Molecule Inhibitors of a Class I Histone Deacetylase from Plasmodium falciparum |
| Author: |
Nguyen, Cokey; Urgaonkar, Sameer; Cortese, Joseph; Barker, Robert H.; Greenberg, Edward; Tang, Weiping; Patel, Vishal; Mazitschek, Ralph; Coleman, Bradley Ian; Bradner, James Elliott; Schreiber, Stuart L.; Duraisingh, Manoj T.; Wirth, Dyann Fergus; Clardy, Jon C.
Note: Order does not necessarily reflect citation order of authors. |
| 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. |
| Full Text & Related Files: |
2669731.pdf (61.80Kb; PDF) 
|
| 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. |
| Published Version: | doi:10.1021/jm801654y |
| Other Sources: | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2669731/pdf/ |
| Terms of Use: | This article is made available under the terms and conditions applicable to Open Access Policy Articles, as set forth at http://nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of-use#OAP |
| Citable link to this page: | http://nrs.harvard.edu/urn-3:HUL.InstRepos:4461121 |
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Peer reviewed scholarly articles from the Faculty of Arts and Sciences of Harvard University
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