A small molecule inhibitor of fungal histone acetyltransferase Rtt109
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Journal ArticlePublication Date
2013-05-15Keywords
Histone AcetyltransferasesSaccharomyces cerevisiae Proteins
Candida albicans
Biochemistry, Biophysics, and Structural Biology
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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.Source
Bioorg Med Chem Lett. 2013 May 15;23(10):2853-9. doi: 10.1016/j.bmcl.2013.03.112. Link to article on publisher's siteDOI
10.1016/j.bmcl.2013.03.112Permanent Link to this Item
http://hdl.handle.net/20.500.14038/29269PubMed ID
23587423Related Resources
Link to Article in PubMedae974a485f413a2113503eed53cd6c53
10.1016/j.bmcl.2013.03.112