Bcr-Abl kinase inhibitor PF-114

{
  "id": "MLC-T-ONC-011924",
  "term": "Bcr-Abl kinase inhibitor PF-114",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, Bcr-Abl tyrosine kinase inhibitor, with potential antineoplastic activity. Designed to overcome resistance of tumor cells to second generation Bcr-Abl inhibitors, PF-114 targets and binds to the Bcr-Abl fusion oncoprotein, including those fusion proteins with the ‘gatekeeper’ resistance mutation T315I, an amino acid substitution at position 315 in Bcr-Abl from a threonine (T) to an isoleucine (I). This inhibits Bcr-Abl-mediated proliferation of, and enhances apoptosis in, Philadelphia chromosome-positive (Ph+) hematologic malignancies. The Bcr-Abl fusion protein is an aberrantly activated tyrosine kinase produced by leukemia cells that contain the Philadelphia chromosome.",
  "synonyms": [
    "Bcr-Abl inhibitor PF-114"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/bcr-abl-kinase-inhibitor-pf-114/"
}