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Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1
Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden..
Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Sprint BioSci AB, Huddinge, Sweden..
Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Univ Strasbourg, Fac Pharm, MEDALIS Drug Discovery Ctr, LFCS,CAMB,UMR7199,CNRS,LIT,UMR7200, F-67401 Illkirch Graffenstaden, France..
Karolinska Inst, Dept Med Biochem & Biophys, Sci Life Lab, Div Translat Med & Chem Biol, Stockholm, Sweden.;Karolinska Inst, Dept Med Biochem & Biophys, Div Translat Med & Chem Biol, Chem Biol Consortium Sweden, Stockholm, Sweden..
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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
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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
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-280245DOI: 10.1021/acs.jmedchem.5b01741ISI: 000370212700023PubMedID: 26771665OAI: oai:DiVA.org:uu-280245DiVA: diva2:910541
Funder
Knut and Alice Wallenberg FoundationSwedish Research CouncilSwedish Cancer SocietyEU, European Research CouncilSwedish Childhood Cancer FoundationGöran Gustafsson Foundation for Research in Natural Sciences and MedicineCarl Tryggers foundation Wenner-Gren FoundationsTorsten Söderbergs stiftelse
Available from: 2016-03-09 Created: 2016-03-09 Last updated: 2017-05-04Bibliographically approved

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Baranczewski, PawelSvensson, RichardArtursson, Per

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