1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2).

Détails

ID Serval
serval:BIB_9DF2682ECDFF
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2).
Périodique
Bioorganic & medicinal chemistry letters
Auteur⸱e⸱s
Röhrig U.F., Majjigapu S.R., Caldelari D., Dilek N., Reichenbach P., Ascencao K., Irving M., Coukos G., Vogel P., Zoete V., Michielin O.
ISSN
1464-3405 (Electronic)
ISSN-L
0960-894X
Statut éditorial
Publié
Date de publication
01/09/2016
Peer-reviewed
Oui
Volume
26
Numéro
17
Pages
4330-4333
Langue
anglais
Notes
Publication types: Journal Article
Publication Status: ppublish
Résumé
Indoleamine 2,3-dioxygenase 2 (IDO2) is a potential therapeutic target for the treatment of diseases that involve immune escape such as cancer. In contrast to IDO1, only a very limited number of inhibitors have been described for IDO2 due to inherent difficulties in expressing and purifying a functionally active, soluble form of the enzyme. Starting from our previously discovered highly efficient 4-aryl-1,2,3-triazole IDO1 inhibitor scaffold, we used computational structure-based methods to design inhibitors of IDO2 which we then tested in cellular assays. Our approach yielded low molecular weight inhibitors of IDO2, the most active displaying an IC50 value of 51μM for mIDO2, and twofold selectivity over hIDO1. These compounds could be useful as molecular probes to investigate the biological role of IDO2, and could inspire the design of new IDO2 inhibitors.

Mots-clé
Cancer immunotherapy, Cellular assays, Indoleamine 2,3-dioxygenase, Molecular modeling, Tryptophan metabolism
Pubmed
Web of science
Création de la notice
05/08/2016 17:36
Dernière modification de la notice
20/08/2019 16:04
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