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Chemical Probes to ...
Chemical Probes to Study ADP-Ribosylation : Synthesis and Biochemical Evaluation of Inhibitors of the Human ADP-Ribosyltransferase ARTD3/PARP3
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- Lindgren, Anders E. G. (author)
- Umeå universitet,Kemiska institutionen
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- Karlberg, Tobias (author)
- Karolinska Institutet
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- Ekblad, Torun (author)
- Karolinska Institutet
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- Spjut, Sara (author)
- Umeå universitet,Kemiska institutionen
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- Thorsell, Ann-Gerd (author)
- Karolinska Institutet
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- Andersson, C. David (author)
- Umeå universitet,Kemiska institutionen
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- Nhan, Ton Tong (author)
- Umeå universitet,Kemiska institutionen
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- Hellsten, Victor (author)
- Umeå universitet,Kemiska institutionen
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Weigelt, Johan (author)
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- Linusson, Anna (author)
- Umeå universitet,Kemiska institutionen
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- Schuler, Herwig (author)
- Karolinska Institutet
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- Elofsson, Mikael (author)
- Umeå universitet,Kemiska institutionen
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(creator_code:org_t)
- 2013-11-22
- 2013
- English.
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In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 56:23, s. 9556-9568
- 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 racemic 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[1-(pyridin-2-yl)ethyl]propanamide, 1, has previously been identified as a potent but unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3). Herein we describe synthesis and evaluation of SS compounds in this class. It was found that the stereochemistry is of great importance for both selectivity and potency and that substituents on the phenyl ring resulted in poor solubility. Certain variations at the meso position were tolerated and caused a large shift in the binding pose. Changes to the ethylene linker that connects the quinazolinone to the amide were also investigated but proved detrimental to binding. By combination of synthetic organic chemistry and structure-based design, two selective inhibitors of ARTD3 were discovered.
Subject headings
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Lindgren, Anders ...
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Karlberg, Tobias
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Ekblad, Torun
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Spjut, Sara
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Thorsell, Ann-Ge ...
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Andersson, C. Da ...
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show more...
-
Nhan, Ton Tong
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Hellsten, Victor
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Weigelt, Johan
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Linusson, Anna
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Schuler, Herwig
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Elofsson, Mikael
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show less...
- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Chemical Science ...
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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 ...
- Articles in the publication
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Journal of Medic ...
- By the university
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Umeå University
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Karolinska Institutet