Preferred Label : PI3K-gamma Inhibitor ZX-4081;
NCIt synonyms : PI3K-g Inhibitor ZX-4081; PI3Kg Inhibitor ZX-4081; PI3Kgamma Inhibitor ZX-4081;
NCIt definition : An orally bioavailable selective inhibitor of the gamma isoform of phosphoinositide-3
kinase (PI3Kg), with potential immunomodulating and antineoplastic activities. Upon
oral administration of PI3Kg inhibitor ZX-4081, this agent targets and inhibits the
PI3Kg isoform and prevents the activation of the PI3Kg-AKT-mediated signaling pathway.
As PI3Kg plays an important role in immune suppression and promotes immunosuppressive
myeloid cell polarization during tumor growth and metastasis, the inhibition of PI3Kg
may abrogate the immune-suppressive nature in the tumor microenvironment (TME) and
impair PI3Kg-AKT-mediated macrophage polarization. This may promote anti-tumor immunity,
may increase CD8-positive T-cell activation and M1-like macrophages and may lead to
a reduction in cellular proliferation in PI3Kg-expressing tumor cells. By selectively
targeting this isoform, PI3K signaling in normal, non-neoplastic cells is minimally
impacted or not affected at all, which minimizes the side effect profile for this
agent. PI3Kg is highly expressed in leukocytes and plays a critical role in activation
of myeloid cells at sites of inflammation and tumorigenesis, T-cell recruitment into
the TME, chemokine-mediated chemotaxis and growth factor signaling.;
Molecule name : ZX 4081; ZX-4081;
NCI Metathesaurus CUI : CL1773731;
Origin ID : C185421;
UMLS CUI : C5666992;
Semantic type(s)
- concept_is_in_subset
- has_target
