Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor

@article{Krytof2005AntiproliferativeAO,
  title={Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor},
  author={Vladim{\'i}r Kry{\vs}tof and Iain W. McNae and Malcolm D. Walkinshaw and Peter M. Fischer and Petr M{\"u}ller and Borivoj Vojtesek and Martin Ors{\'a}g and Libor Havl{\'i}cek and Miroslav Strnad},
  journal={Cellular and Molecular Life Sciences CMLS},
  year={2005},
  volume={62},
  pages={1763-1771}
}
The study describes the protein kinase selectivity profile, as well as the binding mode of olomoucine II in the catalytic cleft of CDK2, as determined from cocrystal analysis. Apart from the main cell cycle-regulating kinase CDK2, olomoucine II exerts specificity for CDK7 and CDK9, with important functions in the regulation of RNA transcription. In vitro anticancer activity of the inhibitor in a panel of tumor cell lines shows a wide potency range with a slight preference for cells harboring a… CONTINUE READING
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