Histone Acetyltransferase
Histone acetyltransferases (HATs) are enzymes that acetylate conserved lysine amino acids on histone proteins by transferring an acetyl group from acetyl CoA to form ε-N-acetyllysine. DNA is wrapped around histones, and, by transferring an acetyl group to the histones, genes can be turned on and off. In general, histone acetylation increases gene expression. HATs are traditionally divided into two different classes based on their subcellular localization. Three important nuclear receptor coactivators that display HAT activity are SRC-1, ACTR, and TIF-2.
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C646是一种histone acetyltransferase(组蛋白乙酰转移酶)抑制剂,抑制p300,Ki为400 nM,比作用于其他乙酰转移酶选择性高。
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MG149是Tip60抑制剂,IC50为74 uM,对MOF的抑制性较相似,IC50为47 uM,而对PCAF和p300则几乎无活性。
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Remodelin氢溴酸盐是乙酰基转移酶NAT10的新型强效选择性抑制剂。
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Anacardic Acid是一个有效的p300 and p300/CBP-associated factor histone acetyltranferases的抑制剂,也具有抗细菌和抗微生物活性,抑制前列腺素合成,并抑制酪氨酸酶和脂肪氧合酶。
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