Publikation: Small Molecule Inhibitors of Human DNA Polymerase λ
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ACS Chemical Biology. 2011, 6(4), pp. 314-319. ISSN 1554-8929. eISSN 1554-8937. Available under: doi: 10.1021/cb100382m
Zusammenfassung
To discover chemical probes to further understand the function of individual DNA polymerases, we established a generally applicable high-throughput screening. By applying this technique we discovered three novel inhibitor classes of human DNA polymerase λ (DNA Pol λ), a key enzyme to maintain the genetic integrity of the genome. The rhodanines, classified as an excellent drug scaffold, were found to be the most potent inhibitors for DNA Pol λ. Importantly, they are up to 10 times less active against the highly similar DNA polymerase β. We investigated basic structure activity relationships. Furthermore, the rhodanines showed pharmacological activity in two human cancer cell lines. So the here reported small molecules could serve as useful DNA Pol λ probes and might serve as starting point to develop novel therapeutic agents.
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STRITTMATTER, Tobias, Bettina BARETH, Timo IMMEL, Thomas HUHN, Thomas U. MAYER, Andreas MARX, 2011. Small Molecule Inhibitors of Human DNA Polymerase λ. In: ACS Chemical Biology. 2011, 6(4), pp. 314-319. ISSN 1554-8929. eISSN 1554-8937. Available under: doi: 10.1021/cb100382mBibTex
@article{Strittmatter2011-04-15Small-12932,
year={2011},
doi={10.1021/cb100382m},
title={Small Molecule Inhibitors of Human DNA Polymerase λ},
number={4},
volume={6},
issn={1554-8929},
journal={ACS Chemical Biology},
pages={314--319},
author={Strittmatter, Tobias and Bareth, Bettina and Immel, Timo and Huhn, Thomas and Mayer, Thomas U. and Marx, Andreas}
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