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Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors
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2017 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 60, no 10, p. 4279-4292Article in journal (Refereed) Published
Abstract [en]

The dCTP pyrophosphatase 1 (dCTPase) is a nucleotide pool "housekeeping" enzyme responsible for the catabolism of canonical and noncanonical nucleoside triphosphates (dNTPs) and has been associated with cancer progression and cancer cell sternness. We have identified a series of piperazin-1-ylpyridazines as a new class of potent dCTPase inhibitors. Lead compounds increase dCTPase thermal and protease stability, display outstanding selectivity over related enzymes and synergize with a cytidine analogue against leukemic cells. This new class of dCTPase inhibitors lays the first stone toward the development of drug-like probes for the dCTPase enzyme.

Place, publisher, year, edition, pages
AMER CHEMICAL SOC , 2017. Vol. 60, no 10, p. 4279-4292
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Medicinal Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-326233DOI: 10.1021/acs.jmedchem.7b00182ISI: 000402498200013PubMedID: 28508636OAI: oai:DiVA.org:uu-326233DiVA, id: diva2:1130647
Funder
Knut and Alice Wallenberg FoundationSwedish Research CouncilEU, European Research CouncilGöran Gustafsson Foundation for Research in Natural Sciences and MedicineSwedish Cancer SocietySwedish Childhood Cancer FoundationTorsten Söderbergs stiftelseRagnar Söderbergs stiftelseAvailable from: 2017-08-10 Created: 2017-08-10 Last updated: 2018-01-13Bibliographically approved

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Mateus, AndréBaranczewski, PawelArtursson, Per

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