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  4. 1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2)
 
research article

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

Rohrig, Ute F.
•
Majjigapu, Somi Reddy  
•
Caldelari, Daniela
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2016
Bioorganic & Medicinal Chemistry Letters

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 51 mu M 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. (C) 2016 Elsevier Ltd. All rights reserved.

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Type
research article
DOI
10.1016/j.bmcl.2016.07.031
Web of Science ID

WOS:000381959900032

Author(s)
Rohrig, Ute F.
Majjigapu, Somi Reddy  
Caldelari, Daniela
Dilek, Nahzli
Reichenbach, Patrick
Ascencao, Kelly
Irving, Melita
Coukos, George
Vogel, Pierre  
Zoete, Vincent
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Date Issued

2016

Publisher

Pergamon-Elsevier Science Ltd

Published in
Bioorganic & Medicinal Chemistry Letters
Volume

26

Issue

17

Start page

4330

End page

4333

Subjects

Indoleamine 2,3-dioxygenase

•

Cancer immunotherapy

•

Molecular modeling

•

Cellular assays

•

Tryptophan metabolism

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
LGSA  
Available on Infoscience
October 18, 2016
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/130286
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