2. Academic Validation
  3. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3

PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3

  • ACS Chem Biol. 2013 Aug 16;8(8):1698-703. doi: 10.1021/cb4002014.
Anders E G Lindgren 1,  Tobias Karlberg,  Ann-Gerd Thorsell,  Mareike Hesse,  Sara Spjut,  Torun Ekblad,  C David Andersson,  Ana Filipa Pinto,  Johan Weigelt,  Michael O Hottiger,  Anna Linusson,  Mikael Elofsson,  Herwig Schüler
Affiliations

Affiliation

  • 1 Department of Chemistry, Umeå University, Umeå, Sweden.
PMID: 23742272 DOI: 10.1021/cb4002014
Abstract

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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-100225
    99.87%, ARTD3/PARP3抑制剂
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