Preferred Label : ARG1/ARG2 Inhibitor OATD-02;
NCIt synonyms : ARG1/2 Inhibitor OATD-02; Arginase 1/2 Inhibitor OATD-02;
NCIt definition : An orally bioavailable boronic acid derivative and inhibitor of arginase 1 (ARG1)
and 2 (ARG2), with potential immunomodulating and antineoplastic activities. Upon
oral administration, ARG1/ARG2 inhibitor OATD-02 selectively inhibits ARG1 and ARG2,
thereby preventing the breakdown of arginine by arginase and restoring arginine levels.
This allows arginine to stimulate the synthesis of nitric oxide (NO) and the secretion
of pro-inflammatory cytokines and chemokines, which induces the proliferation and
activation of T-cells. Therefore, this agent may prevent the immunosuppressive effects
of tumor-infiltrating myeloid cells, inhibit the immunomodulatory effect induced by
regulatory T-cells (Tregs), and promote lymphocyte-mediated immune responses against
tumor cells. In addition, inhibition of ARG-mediated signaling may also kill tumor
cells and decrease tumor cell growth by modulating tumor metabolism. Arginase, a manganese-dependent
enzyme that hydrolyzes the amino acid arginine to form ornithine and urea, is produced
by neutrophils, macrophages and myeloid-derived suppressor cells (MDSC). It plays
a key role in inflammation-associated immunosuppression, tumor immunity, tumor cell
growth and in metabolic pathways. Overexpressed in various types of tumors, its overexpression
correlates with poor prognosis due to diminished arginine levels.;
Molecule name : OATD 02; OAT 1746; OAT-1746; OATD-02;
NCI Metathesaurus CUI : CL1907121;
Origin ID : C200316;
concept_is_in_subset
- has_target
