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Identification of T...
Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1
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- Llona-Minguez, Sabin (author)
- Karolinska Institutet
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- Höglund, Andreas (author)
- Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden.;Sprint BioScience AB, Huddinge, Sweden.
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- Wiita, Elisee (author)
- Karolinska Institutet
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- Almlöf, Ingrid (author)
- Karolinska Institutet
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- Mateus, André (author)
- Uppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab
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- Calderon-Montano, Jose Manuel (author)
- Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden.
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- Cazares-Körner, Cindy (author)
- Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden.
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- Homan, Evert (author)
- Karolinska Institutet
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- Loseva, Olga (author)
- Karolinska Institutet
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- Baranczewski, Pawel (author)
- Uppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab,Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden.
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- Jemth, Ann-Sofie (author)
- Karolinska Institutet
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- Häggblad, Maria (author)
- Stockholms universitet,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab),Univ Stockholm, RNAi Cell Screening Fac, Dept Biochem & Biophys, Sci Life Lab, S-10691 Stockholm, Sweden.
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- Martens, Ulf (author)
- Stockholms universitet,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab),Univ Stockholm, RNAi Cell Screening Fac, Dept Biochem & Biophys, Sci Life Lab, S-10691 Stockholm, Sweden.
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- Lundgren, Bo (author)
- Stockholms universitet,Institutionen för biokemi och biofysik,Science for Life Laboratory (SciLifeLab),Univ Stockholm, RNAi Cell Screening Fac, Dept Biochem & Biophys, Sci Life Lab, S-10691 Stockholm, Sweden.
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- Artursson, Per (author)
- Uppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab
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- Lundbäck, Thomas (author)
- Karolinska Institutet
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- Jenmalm Jensen, Annika (author)
- Karolinska Institutet
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- Warpman Berglund, Ulrika (author)
- Karolinska Institutet
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- Scobie, Martin (author)
- Karolinska Institutet
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- Helleday, Thomas (author)
- Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden.
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Karolinska Institutet Karolinska Inst, Div Translat Med & Chem Biol, Sci Life Lab, Dept Med Biochem & Biophys, S-17121 Stockholm, Sweden;Sprint BioScience AB, Huddinge, Sweden. (creator_code:org_t)
- 2017-02-15
- 2017
- English.
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In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 60:5, s. 2148-2154
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- The dCTP pyrophosphatase 1 (dCTPase) is involved in the regulation of the cellular dNTP pool and has been linked to cancer progression. Here we report on the discovery of a series of 3,6-disubstituted triazolothiadiazoles as potent dCTPase inhibitors. Compounds 16 and 18 display good correlation between enzymatic inhibition and target engagement, together with efficacy in a cellular synergy model, deeming them as a promising starting point for hit -to-lead development.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Llona-Minguez, S ...
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Höglund, Andreas
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Wiita, Elisee
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Almlöf, Ingrid
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Mateus, André
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Calderon-Montano ...
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show more...
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Cazares-Körner, ...
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Homan, Evert
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Loseva, Olga
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Baranczewski, Pa ...
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Jemth, Ann-Sofie
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Häggblad, Maria
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Martens, Ulf
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Lundgren, Bo
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Artursson, Per
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Lundbäck, Thomas
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Jenmalm Jensen, ...
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Warpman Berglund ...
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Scobie, Martin
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Helleday, Thomas
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Medical Biotechn ...
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and Medical Biotechn ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Pharmaceutical S ...
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Journal of Medic ...
- By the university
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Stockholm University
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Uppsala University
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Karolinska Institutet