期刊
DRUG DISCOVERY TODAY
卷 26, 期 11, 页码 2699-2706出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2021.05.011
关键词
NNMT; Nicotinamide; S-adenosyl-L-methionine; Cancer; Metabolic disorder; Neurodegenerative disease
资金
- Chinese Scholarship Council (CSC) [201506270162]
NNMT is an enzyme that methylates nicotinamide to generate 1-methyl nicotinamide, playing roles in human health beyond metabolic functions and contributing to various diseases, including cancers. However, the development of cell-active inhibitors against NNMT still faces challenges and lacks progress.
Nicotinamide N-methyltransferase (NNMT) methylates nicotinamide (NA) to generate 1-methyl nicotinamide. Since its discovery 70 years ago, the appreciation of the role of NNMT in human health has evolved from serving only metabolic functions to also being a driving force in diseases, including a variety of cancers. Despite the increasing evidence indicating NNMT as a viable therapeutic target, the development of cell-active inhibitors against this enzyme is lacking. In this review, we provide an overview of the current status of NNMT inhibitor development, relevant in vitro and in vivo studies, and a discussion of the challenges faced in the development of NNMT inhibitors.
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