CDK4/6 degrader BTX-9341

{
  "id": "MLC-T-ONC-012456",
  "term": "CDK4/6 degrader BTX-9341",
  "field": "Oncology and biomedicine",
  "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).",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/cdk4-6-degrader-btx-9341/"
}