Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase.
Antitumor therapy
Diaryl oalkylhydroxylamines
Dual inhibitor
IDO1 inhibition
IDO2 inhibition
Pan inhibition
TDO inhibition
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:
15 Jan 2019
15 Jan 2019
Historique:
received:
02
08
2018
revised:
06
10
2018
accepted:
05
11
2018
pubmed:
24
11
2018
medline:
8
2
2019
entrez:
24
11
2018
Statut:
ppublish
Résumé
Tryptophan (Trp) catabolizing enzymes play an important and complex role in the development of cancer. Significant evidence implicates them in a range of inflammatory and immunosuppressive activities. Whereas inhibitors of indoleamine 2,3-dioxygenase-1 (IDO1) have been reported and analyzed in the clinic, fewer inhibitors have been described for tryptophan dioxygenase (TDO) and indoleamine 2,3-dioxygenase-2 (IDO2) which also have been implicated more recently in cancer, inflammation and immune control. Consequently the development of dual or pan inhibitors of these Trp catabolizing enzymes may represent a therapeutically important area of research. This is the first report to describe the development of dual and pan inhibitors of IDO1, TDO and IDO2.
Identifiants
pubmed: 30469041
pii: S0223-5234(18)30964-4
doi: 10.1016/j.ejmech.2018.11.010
pmc: PMC6318801
mid: NIHMS1513180
pii:
doi:
Substances chimiques
Anti-Inflammatory Agents
0
Antineoplastic Agents
0
Hydroxylamines
0
IDO1 protein, human
0
IDO2 protein, human
0
Immunologic Factors
0
Indoleamine-Pyrrole 2,3,-Dioxygenase
0
Tryptophan Oxygenase
EC 1.13.11.11
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
455-464Subventions
Organisme : NIGMS NIH HHS
ID : R01 GM086482
Pays : United States
Organisme : NIGMS NIH HHS
ID : R15 GM087291
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM126297
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA191191
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA109542
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM115773
Pays : United States
Informations de copyright
Copyright © 2018 Elsevier Masson SAS. All rights reserved.
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