BCR-ABL inhibitor TGRX-678

{
  "id": "MLC-T-ONC-011922",
  "term": "BCR-ABL inhibitor TGRX-678",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable inhibitor of the tyrosine kinase BCR-ABL fusion oncoprotein, with potential antineoplastic activity. Upon oral administration, BCR-ABL inhibitor TGRX-678 specifically targets and binds to the myristate site at the C-terminal of the kinase domain, which results in the cross-linking of SH3 and SH2 domains to the kinase domain, and locks the kinase in its inactive state. This inhibits the activity of BCR-ABL, including the T315I gatekeeper residue mutation. The binding results in the inhibition of BCR-ABL-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. The BCR-ABL fusion protein tyrosine kinase is an abnormal enzyme produced by leukemia cells that contain the Philadelphia chromosome. The T315I mutation, the most common BCR-ABL mutation, shows resistance to nearly all commonly used tyrosine kinase inhibitors (TKIs).",
  "synonyms": [
    "BCR-ABL1 inhibitor TGRX-678"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/bcr-abl-inhibitor-tgrx-678/"
}