Synthesis and biological activity of splitomicin analogs targeted at human NAD+-dependent histone deacetylases (sirtuins)

M Freitag, J Schemies, T Larsen, K El Gaghlab…

文献索引：Freitag, Marcus; Schemies, Joerg; Larsen, Tim; El Gaghlab, Khattab; Schulz, Felix; Rumpf, Tobias; Jung, Manfred; Link, Andreas Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 12 p. 3669 - 3677

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被引用次数: 20

摘要

Small molecules interfering with posttranslational modification of histones are of interest as tools to study epigenetic regulation of gene transcription. Specifically, drugs that interfere with histone deacetylation could be useful to induce differentiation, growth arrest as well as apoptotic cell death in tumor cells. One class of histone deacetylases is known as sirtuins some of which (Saccharomyces cerevisiae Sir2) are for example inhibited by the lactone ...