Preferred Label : Bosmolisib;
NCIt synonyms : DNA-PK/PI3K-delta Inhibitor BR101801;
NCIt definition : An orally bioavailable inhibitor of phosphoinositide 3-kinase delta (PI3-kinase subunit
delta; PI3K-delta; PI3Kdelta) and DNA-dependent protein kinase (DNA-PK), with potential
antineoplastic and immunomodulating activities. Upon oral administration, bosmolisib
inhibits the activity of both PI3K-delta and DNA-PK. This prevents PI3K-mediated signaling
pathways and may lead to the inhibition of cancer cell growth in PI3K-overexpressing
tumor cells. Specifically, since PI3K regulates c-myc expression, inhibition of PI3K
signaling may lead to a decrease in proliferation of c-myc-expressing tumor cells.
Also, by inhibiting the activity of DNA-PK, bosmolisib interferes with the non-homologous
end joining (NHEJ) process and prevents the repair of DNA double strand breaks (DSBs)
caused by ionizing radiation or chemotherapeutic treatment. This increases chemo-
and radiotherapy cytotoxicity by inhibiting the ability of tumor cells to repair damaged
DNA. The PI3K pathway is upregulated in a variety of tumors and plays an important
role in regulating cancer cell proliferation, growth, and survival. DNA-PK is activated
upon DNA damage and plays a key role in repairing double-stranded DNA breaks. The
enhanced ability of tumor cells to repair DSBs plays a major role in the resistance
of tumor cells to chemo- and radiotherapy. In addition, bosmolisib is able to decrease
Tregs and increase CD8 lymphocytes.;
UNII : FJ5CTS1VNJ;
CAS number : 2055765-77-8;
Molecule name : BR 101801; BR-101801;
NCI Metathesaurus CUI : CL1406238;
Origin ID : C172111;
UMLS CUI : C5417896;
Semantic type(s)
- concept_is_in_subset
