ChemBioChem

Cover image for Vol. 17 Issue 22

Editor: Meghan Campbell; Editorial Board Chairs: Thomas Carell, Donald Hilvert, Barbara Imperiali

Online ISSN: 1439-7633

Associated Title(s): ChemCatChem, ChemMedChem, ChemPhysChem, ChemSusChem

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November 24, 2016

Very Important Paper: Exploring the Potent Inhibition of CTP Synthase by Gemcitabine-5'-Triphosphate

Gregory D. McCluskey, Samy Mohamady, Scott D. Taylor, Stephen L. Bearne*

The nucleoside analogue gemcitabine is used as a chemotherapy drug to treat lung, pancreatic, bladder, and breast cancers. One metabolite of this drug, gemcitabine-5'-triphosphate, is believed to deplete intracellular CTP levels by inhibiting CTP synthase, but the direct inhibition of this enzyme had not been demonstrated. Now, S.L. Bearne (Dalhousie University, Canada) and co-workers show that gemcitabine-5'-triphosphate is indeed a potent competitive inhibitor of Escherichia coli CTP synthase. Remarkably, the enzyme also acts on an abundant catabolite of the drug, 2',2'-difluoro-2'-deoxyuridine-5'-triphosphate, to convert it back to gemcitabine-5'-triphosphate, suggesting that CTP synthase may play a role in replenishing the active drug in vivo.

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