Preferred Label : IDO1/TDO2 Inhibitor DN1406131;
NCIt synonyms : Indoleamine 2,3-Dioxygenase 1/Tryptophan 2,3-Dioxygenase 2 Inhibitor DN1406131;
NCIt definition : An inhibitor of both the enzymes indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1) and tryptophan
2,3-dioxygenase 2 (TDO2; TDO-2), with potential immunomodulating and antineoplastic
activities. Upon administration, IDO1/TDO2 inhibitor DN1406131 targets, binds to and
inhibits both IDO1 and TDO2, which catalyze the first and rate-limiting step in the
production of the immunosuppressive transcription factor aryl hydrocarbon receptor
(AhR) ligand kynurenine (KYN). This inhibits the IDO1/TDO2-KYN-AhR pathway. Abrogation
of AhR activation prevents the activation of immune-tolerant dendritic cells (DCs)
and regulatory T-cells (Tregs) in the tumor microenvironment (TME). This may restore
the immune response against tumor cells in which IDO1 and/or TDO2 are overexpressed.
The IDO1/TDO2-KYN-AhR pathway is overexpressed in a variety of tumor cell types, plays
a key role in immunosuppression and its expression is correlated with poor prognosis.;
Molecule name : DN 1406131; DN-1406131; DN131;
NCI Metathesaurus CUI : CL973340;
Origin ID : C162858;
UMLS CUI : C5206846;
Semantic type(s)
- concept_is_in_subset
- has_target
