Preferred Label : Chk1 Inhibitor PEP07;
NCIt synonyms : Checkpoint Kinase 1 Inhibitor PEP07;
NCIt definition : An orally bioavailable inhibitor of checkpoint kinase 1 (Chk1), with potential antineoplastic
and chemosensitization activities. Upon oral administration, Chk1 inhibitor PEP07
selectively binds to Chk1, thereby preventing Chk1 activity 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. PEP07 may potentiate the cytotoxicity of
DNA-damaging agents and reverse tumor cell resistance to chemotherapeutic agents.
Chk1, an adenosine triphosphate (ATP)-dependent serine/threonine kinase overexpressed
in a variety of cancer cell types, mediates cell cycle checkpoint control and is essential
for DNA repair; it plays a key role in resistance to chemotherapeutic agents by repairing
DNA damage.;
Molecule name : PEP-07; PEP 07;
NCI Metathesaurus CUI : CL1906234;
Origin ID : C199296;
concept_is_in_subset
- has_target
