Inhibitors of nicotinamide N-methyltransferase designed to mimic the methylation reaction transition state

• DOI: 10.1039/c7ob01357d
• Publication Date: 2017-07-24T11:35:59Z
• Authors: Matthijs J. van H...; Rebecca Taig; Jilles Kuppens; Javier Sastre Toraño; Ed E. Moret; Richard B. Parsons; Davide Sartini; Monica Emanuelli; Nathaniel I. Martin
• Keywords: Models, Molecular; Niacinamide; 0301 basic medicine; 03 medical and health sciences; Drug Design; Taverne; Nicotinamide N-Methyltransferase; 500; Humans; Enzyme Inhibitors; 540; 3. Good health

Inhibitors designed to simultaneously occupy the different substrate binding pockets of the NNMT active site reveal key structural features required for potent inhibition.