Zn2Motif-Tethered Short-Chain Fatty Acids as a Novel Class of Histone Deacetylase
申请人:Chen Ching-Shih
公开号:US20070225373A1
公开(公告)日:2007-09-27
Zn
2+
-chelating motif-tethered fatty acids as histone deacetylase (HDAC) inhibitors. One hydroxamate-tethered phenylbutyrate compound, N-hydroxy-4-(4-phenylbutyrylamino)-benzamide (HTPB), displayed nM potency in inhibiting HDAC activity. Exposure of several cancer cell lines to HTPB at sub-μM concentrations showed reduced cell proliferation accompanied by histone hyperacetylation and elevated p21
WAF/CIP1
expression, hallmark features associated with intracellular HDAC inhibition.
Zn2+螯合基固定的脂肪酸作为组蛋白去乙酰化酶(HDAC)抑制剂。一种羟酰胺基固定的苯丁酸化合物,N-羟基-4-(4-苯丁酰氨基)-苯甲酰胺(HTPB),在抑制HDAC活性方面表现出纳摩尔级别的效力。将几种癌细胞系暴露于亚微米浓度的HTPB中,显示出细胞增殖减少,伴随着组蛋白高乙酰化和升高的p21WAF/CIP1表达,这是与细胞内HDAC抑制相关的标志性特征。