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Identification of multidentate tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors that simultaneously access the DNA, protein and catalytic-binding sites by oxime diversification

Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a member of the phospholipase D family that can downregulate the anticancer effects of the type I topoisomerase (TOP1) inhibitors by hydrolyzing the 3′-phosphodiester bond between DNA and the TOP1 residue Y723 in the critical stalled intermediate that is the...

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Detalles Bibliográficos
Autores principales: Zhao, Xue Zhi, Wang, Wenjie, Lountos, George T., Kiselev, Evgeny, Tropea, Joseph E., Needle, Danielle, Pommier, Yves, Burke, Terrence R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10170656/
https://www.ncbi.nlm.nih.gov/pubmed/37181631
http://dx.doi.org/10.1039/d2cb00230b