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Potency boost of a Mycobacterium tuberculosis dihydrofolate reductase inhibitor by multienzyme F(420)H(2)-dependent reduction

Triaza-coumarin (TA-C) is a Mycobacterium tuberculosis (Mtb) dihydrofolate reductase (DHFR) inhibitor with an IC(50) (half maximal inhibitory concentration) of ∼1 µM against the enzyme. Despite this moderate target inhibition, TA-C shows exquisite antimycobacterial activity (MIC(50), concentration i...

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Detalles Bibliográficos
Autores principales: Aragaw, Wassihun Wedajo, Lee, Brendon M., Yang, Xuan, Zimmerman, Matthew D., Gengenbacher, Martin, Dartois, Véronique, Chui, Wai-Keung, Jackson, Colin J., Dick, Thomas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Academy of Sciences 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8237569/
https://www.ncbi.nlm.nih.gov/pubmed/34161270
http://dx.doi.org/10.1073/pnas.2025172118