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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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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Kossmann, Bradley R, Abdelmalak, Monica, Lopez, Sophia, Tender, Gabrielle, Yan, Chunli, Pommier, Yves, Marchand, Christophe, Ivanov, Ivaylo
Formato: Artigo
Idioma:Inglês
Publicado em: 2016
Assuntos:
Acesso em linha: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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