Development of fluorescence polarization-based competition assay for nicotinamide N-methyltransferase.
Fluorescence polarization
High-throughput screening
Inhibitor
Nicotinamide N-Methyltransferase
Protein methyltransferase
Journal
Analytical biochemistry
ISSN: 1096-0309
Titre abrégé: Anal Biochem
Pays: United States
ID NLM: 0370535
Informations de publication
Date de publication:
01 09 2020
01 09 2020
Historique:
received:
12
04
2020
revised:
14
06
2020
accepted:
15
06
2020
pubmed:
6
7
2020
medline:
7
2
2021
entrez:
6
7
2020
Statut:
ppublish
Résumé
Methylation-mediated pathways play important roles in the progression of various diseases. Thus, targeting methyltransferases has proven to be a promising strategy for developing novel therapies. Nicotinamide N-methyltransferase (NNMT) is a major metabolic enzyme involved in epigenetic regulation through catalysis of methyl transfer from the cofactor S-adenosyl-l-methionine onto nicotinamide and other pyridines. Accumulating evidence infers that NNMT is a novel therapeutic target for a variety of diseases such as cancer, diabetes, obesity, cardiovascular and neurodegenerative diseases. Therefore, there is an urgent need to discover potent and specific inhibitors for NNMT to assess its therapeutical potential. Herein, we reported the design and synthesis of a fluorescent probe II138, exhibiting a K
Identifiants
pubmed: 32622979
pii: S0003-2697(20)30365-1
doi: 10.1016/j.ab.2020.113833
pmc: PMC7416818
mid: NIHMS1608963
pii:
doi:
Substances chimiques
Enzyme Inhibitors
0
Fluorescent Dyes
0
NNMT protein, human
EC 2.1.1.1
Nicotinamide N-Methyltransferase
EC 2.1.1.1
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
113833Subventions
Organisme : NCI NIH HHS
ID : P30 CA023168
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM117275
Pays : United States
Organisme : NCI NIH HHS
ID : U01 CA214649
Pays : United States
Informations de copyright
Copyright © 2020 The Author(s). Published by Elsevier Inc. All rights reserved.
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