Identification of potent triazolylpyridine nicotinamide phosphoribosyltransferase (NAMPT) inhibitors bearing a 1,2,3-triazole tail group.
Cancer
Click chemistry
Inhibitors
NAD
Nicotinamide phosphoribosyltransferase
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Nov 2019
01 Nov 2019
Historique:
received:
19
06
2019
revised:
29
07
2019
accepted:
30
07
2019
pubmed:
11
8
2019
medline:
26
11
2019
entrez:
11
8
2019
Statut:
ppublish
Résumé
The enzyme nicotinamide phosphoribosyltransferase is both a key intracellular enzyme for NAD biosynthesis (iNAMPT) and an extracellular cytokine (eNAMPT). The relationship between this latter role and the catalytic activity of the enzyme is at present unknown. With the intent of discovering inhibitors specifically able to target eNAMPT, we increased the polarity of MV78 (EC
Identifiants
pubmed: 31400709
pii: S0223-5234(19)30706-8
doi: 10.1016/j.ejmech.2019.111576
pii:
doi:
Substances chimiques
Cytokines
0
Enzyme Inhibitors
0
Triazoles
0
Nicotinamide Phosphoribosyltransferase
EC 2.4.2.12
nicotinamide phosphoribosyltransferase, human
EC 2.4.2.12
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
111576Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.