期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 10, 页码 2853-2859出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.03.112
关键词
Saccharomyces cerevisiae; Candida albicans; Histone acetyltransferase; Molecular Libraries Probe Production; Centers Network (MLPCN)
资金
- NIH [R21 NS66432, R01 GM055712, F31 AI078726]
The histone acetyltransferase Rtt109 is the sole enzyme responsible for acetylation of histone H3 lysine 56 (H3K56) in fungal organisms. Loss of Rtt109 renders fungal cells extremely sensitive to genotoxic agents, and prevents pathogenesis in several clinically important species. Here, via a high throughput chemical screen of >300,000 compounds, we discovered a chemical inhibitor of Rtt109 that does not inhibit other acetyltransferase enzymes. This compound inhibits Rtt109 regardless of which histone chaperone cofactor protein (Asf1 or Vps75) is present, and appears to inhibit Rtt109 via a tight-binding, uncompetitive mechanism. (C) 2013 Elsevier Ltd. All rights reserved.
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