Preferred Label : CDK4/6 Degrader BTX-9341;
NCIt definition : An orally bioavailable bifunctional degrader of cyclin-dependent kinase (CDK) types
4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon oral administration,
CDK4/6 degrader BTX-9341 targets and binds to CDK4 and CDK6, as well as cereblon (CRBN),
a component of the CRL4-CRBN E3 ubiquitin ligase complex that directs proteins for
destruction. This leads to ubiquitination and induces proteasome-mediated degradation
of CDK4 and CDK6, thereby inhibiting the phosphorylation of retinoblastoma protein
(Rb) early in the G1 phase, preventing CDK-mediated G1-S-phase transition and leading
to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation.
CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types
and play a key role in the regulation of both cell cycle progression from the G1-phase
into the S-phase and tumor cell proliferation. BTX-9341 is able to penetrate through
the blood-brain barrier (BBB).;
Molecule name : BTX-9341; BTX 9341;
Origin ID : C211667;
concept_is_in_subset
- has_target
