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

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

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

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Bibliographic Details
Main Authors: Matthijs J. van Haren, Yongzhi Gao, Ned Buijs, Roberto Campagna, Davide Sartini, Monica Emanuelli, Lukasz Mateuszuk, Agnieszka Kij, Stefan Chlopicki, Pol Escudé Martinez de Castilla, Raymond Schiffelers, Nathaniel I. Martin
Format: Article
Language:English
Published: MDPI AG 2021-09-01
Series:Biomolecules
Subjects:
NNMT
inhibition
prodrug
cell permeability
esterase
cellular activity
Online Access:https://www.mdpi.com/2218-273X/11/9/1357

Internet

https://www.mdpi.com/2218-273X/11/9/1357

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