Merck

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

Bioorganic & medicinal chemistry letters (2009-12-17)
Alexander C Roy, Faylene A Lunn, Stephen L Bearne
RESUMO

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.

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