Novel Inhibitors of Nicotinamide-N-Methyltransferase for the Treatment of Metabolic Disorders

Nicotinamide-N-methyltransferase (NNMT) is a cytosolic enzyme catalyzing the transfer of a methyl group from S-adenosyl-methionine (SAM) to nicotinamide (Nam). It is expressed in many tissues including the liver, adipose tissue, and skeletal muscle. Its expression in several cancer cell lines has be...

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Detalles Bibliográficos
Autores principales: Kannt, Aimo, Rajagopal, Sridharan, Hallur, Mahanandeesha S., Swamy, Indu, Kristam, Rajendra, Dhakshinamoorthy, Saravanakumar, Czech, Joerg, Zech, Gernot, Schreuder, Herman, Ruf, Sven
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7918612/
https://www.ncbi.nlm.nih.gov/pubmed/33668468
http://dx.doi.org/10.3390/molecules26040991
Descripción
Sumario:Nicotinamide-N-methyltransferase (NNMT) is a cytosolic enzyme catalyzing the transfer of a methyl group from S-adenosyl-methionine (SAM) to nicotinamide (Nam). It is expressed in many tissues including the liver, adipose tissue, and skeletal muscle. Its expression in several cancer cell lines has been widely discussed in the literature, and recent work established a link between NNMT expression and metabolic diseases. Here we describe our approach to identify potent small molecule inhibitors of NNMT featuring different binding modes as elucidated by X-ray crystallographic studies.

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