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  • Lindgren, Anders E. G.Umeå universitet,Kemiska institutionen (author)

PARP Inhibitor with Selectivity Toward ADP-Ribosyltransferase ARTD3/PARP3

  • Article/chapterEnglish2013

Publisher, publication year, extent ...

  • 2013-06-25
  • American Chemical Society (ACS),2013
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:umu-81013
  • https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-81013URI
  • https://doi.org/10.1021/cb4002014DOI
  • http://kipublications.ki.se/Default.aspx?queryparsed=id:127303102URI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • Inhibiting ADP-ribosyl transferases with PARP-inhibitors is considered a promising strategy for the treatment of many cancers and ischemia, but most of the cellular targets are poorly characterized. Here, we describe an inhibitor of ADP-ribosyltransferase-3/poly(ADP-ribose) polymerase-3 (ARTD3), a regulator of DNA repair and mitotic progression. In vitro profiling against 12, members of the enzyme family suggests selectivity for ARTD3, and crystal structures illustrate the molecular basis for inhibitor selectivity. The compound is active in cells, where it elicits ARTD3-specific effects at submicromolar concentration. Our results show that by targeting the nicotinamide binding site, selective inhibition can be achieved among the closest relatives of the validated clinical target, ADP-ribosyltransferase-1/poly(ADP-ribose) polymerase-1.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

  • Karlberg, TobiasKarolinska Institutet (author)
  • Thorsell, Ann-GerdKarolinska Institutet (author)
  • Hesse, Mareike (author)
  • Spjut, SaraUmeå universitet,Kemiska institutionen(Swepub:umu)saaspt99 (author)
  • Ekblad, TorunKarolinska Institutet (author)
  • Andersson, C. DavidUmeå universitet,Kemiska institutionen(Swepub:umu)dadaon01 (author)
  • Pinto, Ana FilipaKarolinska Institutet (author)
  • Weigelt, Johan (author)
  • Hottiger, Michael O. (author)
  • Linusson, AnnaUmeå universitet,Kemiska institutionen(Swepub:umu)analin99 (author)
  • Elofsson, MikaelUmeå universitet,Kemiska institutionen(Swepub:umu)miel0001 (author)
  • Schueler, HerwigKarolinska Institutet (author)
  • Umeå universitetKemiska institutionen (creator_code:org_t)

Related titles

  • In:ACS Chemical Biology: American Chemical Society (ACS)8:8, s. 1698-17031554-89291554-8937

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