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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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Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:Bioorg Med Chem Lett
Prif Awduron: Kossmann, Bradley R, Abdelmalak, Monica, Lopez, Sophia, Tender, Gabrielle, Yan, Chunli, Pommier, Yves, Marchand, Christophe, Ivanov, Ivaylo
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: 2016
Pynciau:
Mynediad Ar-lein: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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