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Discovery of a novel and selective Indoleamine 2,3-Dioxygenase (IDO-1) inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and its characterization as a potential clinical candidate

Abstract:

Tumors use tryptophan-catabolizing enzymes such as indoleamine 2,3-dioxygenase (IDO-1) to induce an immunosuppressive environment. IDO-1 is induced in response to inflammatory stimuli and promotes immune tolerance through effector T-cell anergy and enhanced Treg function. As such, IDO-1 is a nexus for the induction of a key immunosuppressive mechanism and represents an important immunotherapeutic target in oncology. Starting from HTS hit 5, IDO-1 inhibitor 6 (EOS200271/PF-06840003) has been d...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted manuscript

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Files:
Publisher copy:
10.1021/acs.jmedchem.7b00974

Authors


Crosignani, S More by this author
Bingham, P More by this author
Bottemanne, P More by this author
Cannelle, H More by this author
Cauwenberghs, S More by this author
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European Fund for Economic and Regional Development More from this funder
Walloon Region of Belgium More from this funder
Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
60
Issue:
23
Pages:
9617–9629
Publication date:
2017-11-07
Acceptance date:
2017-11-06
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pubs id:
pubs:809044
URN:
uri:9110a222-b5ef-4b52-adea-6a4da2073d31
UUID:
uuid:9110a222-b5ef-4b52-adea-6a4da2073d31
Local pid:
pubs:809044
Language:
English

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