Novel Inhibitors of Nicotinamide-N-Methyltransferase for the Treatment of Metabolic Disorders
| العنوان: | Novel Inhibitors of Nicotinamide-N-Methyltransferase for the Treatment of Metabolic Disorders |
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| المؤلفون: | Indu N. Swamy, Mahanandeesha S. Hallur, Saravanakumar Dhakshinamoorthy, Rajendra Kristam, Sven Ruf, Aimo Kannt, Sridharan Rajagopal, Gernot Zech, Herman Schreuder, Joerg Czech |
| المساهمون: | Publica |
| المصدر: | Molecules Volume 26 Issue 4 Molecules, Vol 26, Iss 991, p 991 (2021) |
| بيانات النشر: | Multidisciplinary Digital Publishing Institute, 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | Models, Molecular, Niacinamide, Pharmaceutical Science, Adipose tissue, nicotinamide, Nicotinamide N-methyltransferase, Ligands, Article, Analytical Chemistry, Substrate Specificity, lcsh:QD241-441, X-ray, 03 medical and health sciences, chemistry.chemical_compound, Mice, 0302 clinical medicine, lcsh:Organic chemistry, Metabolic Diseases, Drug Discovery, medicine, Nicotinamide N-Methyltransferase, Animals, Humans, nicotinamide-N-methyltransferase, Physical and Theoretical Chemistry, Enzyme Inhibitors, 030304 developmental biology, chemistry.chemical_classification, 0303 health sciences, Binding Sites, Nicotinamide, Organic Chemistry, Skeletal muscle, small molecule inhibitor, metabolic disease, Small molecule, High-Throughput Screening Assays, Rats, Cytosol, medicine.anatomical_structure, Enzyme, chemistry, Biochemistry, Chemistry (miscellaneous), 030220 oncology & carcinogenesis, Microsomes, Liver, Molecular Medicine, Cancer cell lines |
| الوصف: | 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. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1420-3049 |
| DOI: | 10.3390/molecules26040991 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::304d1f534180ae4303006d998f29ee1a |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....304d1f534180ae4303006d998f29ee1a |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14203049 |
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| DOI: | 10.3390/molecules26040991 |