학술논문

Novel Inhibitors of Nicotinamide-N-Methyltransferase for the Treatment of Metabolic Disorders
Document Type
article
Source
Molecules, Vol 26, Iss 4, p 991 (2021)
Subject
nicotinamide-N-methyltransferase
small molecule inhibitor
nicotinamide
metabolic disease
X-ray
Organic chemistry
QD241-441
Language
English
ISSN
1420-3049
Abstract
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.