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Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1
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Number of Authors: 29
2016 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 59, no 3, 1140-1148 p.Article in journal (Refereed) Published
Abstract [en]

The dCTPase pyrophosphatase 1 (dCTPase) regulates the intracellular nucleotide pool through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs). dCTPase is highly expressed in multiple carcinomas and is associated with cancer cell sternness. Here we report on the development of the first potent and selective dCTPase inhibitors that enhance the cytotoxic effect of cytidine analogues in leukemia cells. Boronate 30 displays a promising in vitro ADME profile, including plasma and mouse microsomal half-lives, aqueous solubility, cell permeability and CYP inhibition, deeming it a suitable compound for in vivo studies.

Place, publisher, year, edition, pages
2016. Vol. 59, no 3, 1140-1148 p.
National Category
Biochemistry and Molecular Biology Medicinal Chemistry
URN: urn:nbn:se:su:diva-128185DOI: 10.1021/acs.jmedchem.5b01741ISI: 000370212700023PubMedID: 26771665OAI: diva2:914136
Available from: 2016-03-23 Created: 2016-03-21 Last updated: 2016-03-23Bibliographically approved

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Claesson, MagnusStenmark, Pål
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Department of Biochemistry and Biophysics
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