CDK2 inhibitor ARTS-021

{
  "id": "MLC-T-ONC-012441",
  "term": "CDK2 inhibitor ARTS-021",
  "field": "Oncology and biomedicine",
  "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.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/cdk2-inhibitor-arts-021/"
}