本探讨中,我们第一次发现豆香素类代表抗生素新生霉素(novobiocin)能够直接干扰HIF1α的C端转录活性结构域(CTAD)与p300半胱氨酸组氨酸富集区(CH1)的结合,进而下调HIF1下游基因,尤其是与肿瘤发生密切相关的碳酸酐酶IX (carbonichydrase IX...
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酪氨酸576和酪氨酸577处于激酶结构域的激活环,这些残基的突变减弱FAK的催化活性(6)。
Tyr576 and Tyr577 lie in the activation loop of the kinase domain, and mutation of these residues reduces FAK catalytic activity (6).
和LSD1相似的是,其高度保守的SWIR M结构域是其酶活性所必需的。
Like LSD1, the highly conserved SWIRMdomain is required for its enzymatic activity.
极光激酶A催化结构域苏氨酸(288位)的磷酸化能够增强激酶的活性。
Phosphorylation of Aurora A at Thr288 in its catalytic domain increases kinase activity.
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