黄嘌呤和尿酸对大肠杆菌 CTP 合酶的抑制作用。
Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids.
机构信息
Department of Biochemistry and Molecular Biology, Dalhousie University, Halifax, Nova Scotia, Canada B3H 1X5.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):141-4. doi: 10.1016/j.bmcl.2009.11.017. Epub 2009 Nov 12.
CTP synthase (CTPS) catalyzes the conversion of UTP to CTP and is a recognized target for the development of anticancer, antiviral, and antiprotozoal agents. Xanthine and related compounds inhibit CTPS activity (IC(50)=0.16-0.58mM). The presence of an 8-oxo function (i.e., uric acids) enhances inhibition (IC(50)=0.060-0.121mM). An intact purine ring with anionic character favors inhibition. In general, methylation of the purine does not significantly affect inhibition.
CTP 合酶（CTPS）催化 UTP 转化为 CTP，是开发抗癌、抗病毒和抗原生动物药物的公认靶点。黄嘌呤和相关化合物抑制 CTPS 活性（IC（50）=0.16-0.58mM）。8-氧功能（即尿酸）的存在增强了抑制作用（IC（50）=0.060-0.121mM）。具有阴离子特性的完整嘌呤环有利于抑制。一般来说，嘌呤的甲基化不会显著影响抑制作用。
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