Preferred Label : CDK2 Inhibitor ARTS-021;
NCIt definition : An orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential
antineoplastic activity. Upon oral administration, CDK2 inhibitor ARTS-021 selectively
targets, reversibly binds to and inhibits the activity of the CDK2/CyclinE1 (CCNE1;
CCNE-1) complex. This inhibits retinoblastoma (Rb) phosphorylation and blocks G1/S
transition, which leads to cell cycle arrest, the induction of apoptosis, and the
inhibition of proliferation in CDK2 and/or CCNE1-overexpressing tumor cells. CDK2,
a serine/threonine kinase that plays an important role in the regulation of cell cycle
progression and cellular proliferation, is overexpressed in certain tumor cells. CCNE1,
a regulatory factor and activator of CDK2 is overexpressed in various tumor cell types
and CCNE1 overexpression elevates the activity of CDK2.;
Molecule name : ARTS 021; ARTS-021;
Origin ID : C201128;
concept_is_in_subset
- has_target
