Preferred Label : CDK2 Degrader NKT3964;
NCIt synonyms : PROTAC CDK2 Degrader NKT3964; Proteolysis-targeting Chimera Protein Degrader NKT3964;
NCIt definition : An orally bioavailable, targeted degrader composed of an E3 ubiquitin ligase-binding
moiety that is conjugated, via a linker, to a cyclin-dependent kinase 2 (CDK2)-binding
moiety using the proteolysis targeting chimera (PROTAC) technology, with potential
antineoplastic activity. Upon oral administration of CDK2 degrader NKT3964, the CDK2-binding
moiety specifically targets and binds to CDK2 on tumor cells while the E3 ubiquitin
ligase-binding moiety targets and binds to E3 ubiquitin ligase, thereby creating a
ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation
of CDK2, and inhibits the activity of CDK2. This inhibits retinoblastoma (Rb) phosphorylation
and blocks G1/S transition, which leads to cell cycle arrest, the induction of apoptosis,
and the inhibition of tumor cell proliferation. CDK2, in complex with cyclin E1 (CCNE1;
CCNE-1), phosphorylates Rb, which leads to E2F target gene expression and G1 to S-phase
cell cycle progression. CDK2 and CCNE1 are overexpressed in various tumor cell types.
NKT3964 does not cause cyclin E accumulation.;
Molecule name : NKT-3964; NKT 3964;
Origin ID : C213380;
concept_is_in_subset
- has_target
