Esterase-Sensitive Prodrugs of a Potent Bisubstrate Inhibitor of Nicotinamide N-Methyltransferase (NNMT) Display Cellular Activity

A recently discovered bisubstrate inhibitor of Nicotinamide N-methyltransferase (NNMT) was found to be highly potent in biochemical assays with a single digit nanomolar IC(50) value but lacking in cellular activity. We, here, report a prodrug strategy designed to translate the observed potent bioche...

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Detalles Bibliográficos
Autores principales: van Haren, Matthijs J., Gao, Yongzhi, Buijs, Ned, Campagna, Roberto, Sartini, Davide, Emanuelli, Monica, Mateuszuk, Lukasz, Kij, Agnieszka, Chlopicki, Stefan, Escudé Martinez de Castilla, Pol, Schiffelers, Raymond, Martin, Nathaniel I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8466754/
https://www.ncbi.nlm.nih.gov/pubmed/34572571
http://dx.doi.org/10.3390/biom11091357

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8466754/
https://www.ncbi.nlm.nih.gov/pubmed/34572571
http://dx.doi.org/10.3390/biom11091357

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