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Mechanisms and inhibitors of nicotinamide N-methyltransferase

Journal

RSC MEDICINAL CHEMISTRY
Volume 12, Issue 8, Pages 1254-1261

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d1md00016k

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Funding

  1. Ralph W. and Grace M. Showalter Trust
  2. Department of Medicinal Chemistry and Molecular Pharmacology at Purdue University

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Nicotinamide N-methyltransferase (NNMT) plays a crucial role in regulating methylation potential and nicotinamide degradation in various biological processes. Aberrant expression of NNMT is associated with multiple diseases, leading to a growing interest in evaluating NNMT as a potential therapeutic target and developing NNMT inhibitors. Recent research has focused on understanding NNMT mechanisms, inhibitors, and future directions for drug development.
Nicotinamide N-methyltransferase (NNMT) plays an important role in diverse biological processes by regulating methylation potential and the degradation of nicotinamide. Meanwhile, the aberrant expression of NNMT has been implicated in multiple cancers, metabolic and liver diseases. Therefore, there has been an emerging interest in assessing NNMT as a potential therapeutic target and discovering NNMT inhibitors over the past 5 years. Herein, we focus on the recognition, mechanism, and inhibitors of NNMT with emphasis on key advancements in the field. We also discuss future directions for the development of NNMT inhibitors.

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