Bioorganic & Medicinal Chemistry Letters 2010-01-01

Inhibition of CTP synthase from Escherichia coli by xanthines and uric acids.

Alexander C Roy, Faylene A Lunn, Stephen L Bearne

文献索引：Bioorg. Med. Chem. Lett. 20 , 141-4, (2010)

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摘要

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.Copyright 2009 Elsevier Ltd. All rights reserved.