6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site

M Ghizzoni, J Wu, T Gao, HJ Haisma, FJ Dekker…

文献索引：Ghizzoni, Massimo; Wu, Jiang; Gao, Tielong; Haisma, Hidde J.; Dekker, Frank J.; George Zheng European Journal of Medicinal Chemistry, 2012 , vol. 47, # 1 p. 337 - 344

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被引用次数: 23

摘要

Histone acetyltransferases are important enzymes that regulate various cellular functions, such as epigenetic control of DNA transcription. Development of HAT inhibitors with high selectivity and potency will provide powerful mechanistic tools for the elucidation of the biological functions of HATs and may also have pharmacological value for potential new therapies. In this work, analogs of the known HAT inhibitor anacardic acid were ...