Discovery of selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft

Tyrosyl-DNA phosphodiesterase 2 (TDP2) processes protein/DNA adducts resulting from abortive DNA topoisomerase II (Top2) activity. TDP2 inhibition could provide synergism with the Top2 poison class of chemotherapeutics. By virtual screening of the NCI diversity small molecule database, we identified...

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I publikationen:Bioorg Med Chem Lett
Huvudupphovsmän: Kossmann, Bradley R, Abdelmalak, Monica, Lopez, Sophia, Tender, Gabrielle, Yan, Chunli, Pommier, Yves, Marchand, Christophe, Ivanov, Ivaylo
Materialtyp: Artigo
Språk:Inglês
Publicerad: 2016
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Article
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC4939481/
https://ncbi.nlm.nih.gov/pubmed/27262595
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.05.065
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