Mithramycin 2′-Oximes with Improved Selectivity, Pharmacokinetics, and Ewing Sarcoma Antitumor Efficacy

Mithramycin A (MTM) inhibits the oncogenic transcription factor EWS-FLI1 in Ewing sarcoma, but poor pharmacokinetics (PK) and toxicity limit its clinical use. To address this limitation, we report an efficient MTM 2′-oxime (MTM(ox)) conjugation strategy for rapid MTM diversification. Comparative cyt...

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Publicado en:J Med Chem
Main Authors: Liu, Yang, Eckenrode, Joseph M., Zhang, Yinan, Zhang, Jianjun, Hayden, Reiya C., Kyomuhangi, Annet, Ponomareva, Larissa V., Cui, Zheng, Rohr, Jürgen, Tsodikov, Oleg V., Van Lanen, Steven G., Shaaban, Khaled A., Leggas, Markos, Thorson, Jon S.
Formato: Artigo
Idioma:Inglês
Publicado: 2020
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC7810150/
https://ncbi.nlm.nih.gov/pubmed/33191745
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c01526
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