Structure–activity studies on splitomicin derivatives as sirtuin inhibitors and computational prediction of binding mode

RC Neugebauer, U Uchiechowska…

文献索引：Neugebauer, Robert C.; Uchiechowska, Urszula; Meier, Rene; Hruby, Henning; Valkov, Vassil; Verdin, Eric; Sippl, Wolfgang; Jung, Manfred Journal of Medicinal Chemistry, 2008 , vol. 51, # 5 p. 1203 - 1213

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被引用次数: 132

摘要

NAD+-dependent histone deacetylases (sirtuins) are enzymes that cleave acetyl groups from lysines in histones and other proteins. Potent selective sirtuin inhibitors are interesting tools for the investigation of the biological functions of those enzymes and may be future drugs for the treatment of cancer. Splitomicin was among the first two inhibitors that were discovered for yeast sirtuins but showed rather weak inhibition on human enzymes. We ...