Publication: PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3
PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3
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Lindgren, A. E. G., Karlberg, T., Thorsell, A.-G., Hesse, M., Spjut, S., Ekblad, T., Andersson, C. D., Pinto, A. F., Weigelt, J., Hottiger, M. O., Linusson, A., Elofsson, M., & Schüler, H. (2013). PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chemical Biology, 8(8), 1698–1703. https://doi.org/10.1021/cb4002014
Abstract
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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 acti
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- Lindgren, Anders E G
- Karlberg, Tobias
- Thorsell, Ann-Gerd
- Hesse, Mareike
- Spjut, Sara
- Ekblad, Torun
- Andersson, C David
- Pinto, Ana Filipa
- Weigelt, Johan
- Hottiger, Michael O
- Linusson, Anna
- Elofsson, Mikael
- Schüler, Herwig
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Lindgren, A. E. G., Karlberg, T., Thorsell, A.-G., Hesse, M., Spjut, S., Ekblad, T., Andersson, C. D., Pinto, A. F., Weigelt, J., Hottiger, M. O., Linusson, A., Elofsson, M., & Schüler, H. (2013). PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chemical Biology, 8(8), 1698–1703. https://doi.org/10.1021/cb4002014
