MLchartDataset catalogue

BTK degrader UBX-303061

Term · Oncology and biomedicine · MLC-T-ONC-012142

An orally bioavailable chimeric degrader of Bruton's tyrosine kinase (BTK) comprised of an E3 ubiquitin ligase ligand conjugated to a BTK-binding ligand, with potential antineoplastic activity. Upon oral administration, BTK degrader UBX-303061 specifically targets and binds, with its BTK-targeting moiety, to BTK and the E3 ubiquitin ligase ligand moiety binds to E3 ubiquitin ligase. This catalyzes ubiquitination and proteasome-mediated degradation of BTK, and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents B-cell activation 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 B-lymphocyte development, activation, signaling, proliferation and survival.

Table 1. Record
IdentifierMLC-T-ONC-012142
FieldOncology and biomedicine
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-012142",
  "term": "BTK degrader UBX-303061",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable chimeric degrader of Bruton's tyrosine kinase (BTK) comprised of an E3 ubiquitin ligase ligand conjugated to a BTK-binding ligand, with potential antineoplastic activity. Upon oral administration, BTK degrader UBX-303061 specifically targets and binds, with its BTK-targeting moiety, to BTK and the E3 ubiquitin ligase ligand moiety binds to E3 ubiquitin ligase. This catalyzes ubiquitination and proteasome-mediated degradation of BTK, and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents B-cell activation 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 B-lymphocyte development, activation, signaling, proliferation and survival.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/btk-degrader-ubx-303061/"
}

Record 3,915 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.