BCR-ABL Inhibitor TGRX-678

Preferred Label : BCR-ABL Inhibitor TGRX-678;

NCIt synonyms : BCR-ABL1 Inhibitor TGRX-678;

NCIt 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).;

Molecule name : TGRX 678; TGRX-678;

Details

Origin ID

C202237;

chemical_or_drug_has_mechanism_of_action
- Receptor Tyrosine Kinase Inhibition [NCIt concept]
chemical_or_drug_has_physiologic_effect
- Inhibition of Cell Proliferation [NCIt concept]
- Signal Transduction Inhibition [NCIt concept]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP Terminology [NCIt concept]
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- BCR/ABL1 Fusion Protein [NCIt concept]

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