Preferred Label : PI3K-gamma Inhibitor HS248;
NCIt synonyms : PI3Kg Inhibitor HS248;
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, PI3Kg inhibitor HS248 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 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 : HS-248; HS 248;
NCI Metathesaurus CUI : CL1907107;
Origin ID : C200294;
UMLS CUI : C5854511;
Semantic type(s)
- concept_is_in_subset
- has_target
