Scientific article
English

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

Published inBioorganic & medicinal chemistry letters, vol. 26, no. 17, p. 4330-4333
Publication date2016-09-01
First online date2016-07-16
Abstract

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.

Keywords
  • Cancer immunotherapy
  • Cellular assays
  • Indoleamine 2,3-dioxygenase
  • Molecular modeling
  • Tryptophan metabolism
Affiliation entities Not a UNIGE publication
Citation (ISO format)
RÖHRIG, Ute F et al. 1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2). In: Bioorganic & medicinal chemistry letters, 2016, vol. 26, n° 17, p. 4330–4333. doi: 10.1016/j.bmcl.2016.07.031
Main files (1)
Article (Published version)
accessLevelRestricted
Identifiers
Journal ISSN0960-894X
8views
0downloads

Technical informations

Creation28/11/2025 17:14:33
First validation17/02/2026 16:51:22
Update17/02/2026 16:51:22
Status update17/02/2026 16:51:22
Last indexation17/02/2026 16:51:23
All rights reserved by Archive ouverte UNIGE and the University of GenevaunigeBlack