Preferred Label : Chk1 Inhibitor BBI-355;
NCIt definition : An orally bioavailable small molecule inhibitor of checkpoint kinase 1 (chk1), with
potential antineoplastic and chemosensitization activities. Upon oral administration,
chk1 inhibitor BBI-355 selectively binds to chk1, thereby preventing activity of chk1
and abrogating the repair of damaged DNA. This may lead to an accumulation of damaged
DNA, inhibition of cell cycle arrest, and induction of apoptosis. BBI-355 may potentiate
the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapeutic
agents by targeting extrachromosomal DNA (ecDNA) originating from oncogene amplified
cancer cells. Cancer cells that rely on oncogene amplification to grow and survive
are highly sensitive to chk1 inhibition. Chk1, an ATP-dependent serine/threonine kinase,
mediates cell cycle checkpoint control, is essential for DNA repair, and plays a key
role in resistance to chemotherapeutic agents.;
Molecule name : BBI-355; BBI 355;
NCI Metathesaurus CUI : CL1907318;
Origin ID : C200039;
UMLS CUI : C5854459;
Semantic type(s)
- concept_is_in_subset
- has_target
