Preferred Label : IDO/TDO Inhibitor LY-01013;
NCIt definition : An orally bioavailable, small-molecule inhibitor of indoleamine 2,3-dioxygenase 1
(IDO1; IDO-1) and the kynurenine-producing hepatic enzyme tryptophan 2,3-dioxygenase
(TDO), with potential immunomodulating and antineoplastic activities. Upon administration,
IDO1/TDO inhibitor LY-01013 specifically targets and binds to both IDO1, a cytosolic
enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive
metabolite kynurenine, and TDO, a hepatic enzyme catalyzing the first step of tryptophan
degradation. By inhibiting IDO1 and TDO, LY-01013 decreases kynurenine levels in tumor
cells, restores tryptophan and promotes the proliferation and activation of various
immune cells, including dendritic cells (DCs), natural killer (NK) cells and T-lymphocytes.
This reduces the number of tumor-associated regulatory T-cells (Tregs) and activates
the immune system to induce a cytotoxic T-lymphocyte (CTL) response against the IDO1/TDO-expressing
tumor cells, thereby inhibiting the growth of the tumor cells. IDO1 and TDO, both
overexpressed by multiple tumor cell types, play important roles in immunosuppression
and the promotion of tumor cell survival and proliferation. Tryptophan depletion inhibits
T-lymphocyte proliferation and activation, and subsequently suppresses the immune
system.;
Molecule name : LY-01013; LY 01013; LPM 3480226; LPM-3480226;
NCI Metathesaurus CUI : CL1405462;
Origin ID : C171343;
UMLS CUI : C5417853;
Semantic type(s)
- concept_is_in_subset
