Preferred Label : IDO1/TDO2 Inhibitor M4112;
NCIt synonyms : Indoleamine 2,3-Dioxygenase-1/Tryptophan 2,3-Dioxygenase 2 Inhibitor M4112; MS201408-0005;
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 M4112 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 and abrogates AhR activation.
This prevents the activation of immune-tolerant dendritic cells (DCs) and regulatory
T-cells (Tregs) in the tumor microenvironment (TME), and may restore the immune response
by stimulating a cytotoxic T-lymphocyte (CTL) 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 and plays a key role in immunosuppression. Its expression
is correlated with poor prognosis.;
Molecule name : M 4112; M-4112;
NCI Metathesaurus CUI : CL1378711;
Origin ID : C168808;
UMLS CUI : C5239133;
Semantic type(s)
- concept_is_in_subset
- has_target
