期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 8, 页码 2185-2187出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm801654y
关键词
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资金
- U.S. Public Health Service
- NIH [R21NS053660, R21NS059404]
- Medicines for Malaria Venture. Harvard Malaria Initiative [2737380]
- Broad Institute of MIT and Harvard
- Burroughs Welcome Fund
- Humanitarian Assistance for Neglected Diseases (HAND)
- Initiative of Genzyme Corporation
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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