BTK inhibitor TT-01488
Term · Oncology and biomedicine · MLC-T-ONC-012154
An orally bioavailable reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon oral administration, BTK inhibitor TT-01488 non-covalently binds to and inhibits the activity of BTK, including the C481S mutated form, a resistance mutation in the BTK active site in which cysteine is substituted for serine at residue 481. This prevents the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B lymphocytes. BTK C481S mutation plays an important role in resistance to certain BTK inhibitors.
| Identifier | MLC-T-ONC-012154 |
|---|---|
| Field | Oncology and biomedicine |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-012154",
"term": "BTK inhibitor TT-01488",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon oral administration, BTK inhibitor TT-01488 non-covalently binds to and inhibits the activity of BTK, including the C481S mutated form, a resistance mutation in the BTK active site in which cysteine is substituted for serine at residue 481. This prevents the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B lymphocytes. BTK C481S mutation plays an important role in resistance to certain BTK inhibitors.",
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/btk-inhibitor-tt-01488/"
}
Record 3,928 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.