MLchartDataset catalogue

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.

Table 1. Record
IdentifierMLC-T-ONC-012154
FieldOncology and biomedicine
ReferencesNational 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.