Preferred Label : IDO/TDO Inhibitor HTI-1090;
NCIt definition : An orally available 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
HTI-1090 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, HTI-1090 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 : HTI 1090; SHR9146; HTI-1090;
NCI Metathesaurus CUI : CL553173;
Origin ID : C151945;
UMLS CUI : C4726570;
Semantic type(s)
- concept_is_in_subset
