MLchartDataset catalogue

androgen receptor inhibitor ONCT-534

Term · Oncology and biomedicine · MLC-T-ONC-010078

An orally bioavailable dual-action androgen receptor (AR) inhibitor, with potential antineoplastic activity. Upon oral administration, AR inhibitor ONCT-534 targets and binds to both the ligand-binding domain (LBD) and the N-terminal domain (NTD) of the AR, and inhibits AR-mediated signaling and induces the degradation of AR and AR splice variant (AR-SV) proteins. This may inhibit cell growth in AR-overexpressing tumor cells, including those with AR amplification, mutations in the AR LBD, and AR-SVs with loss of the AR LBD. AR is overexpressed in prostate cancers and is involved in the proliferation, survival and chemoresistance of tumor cells.

Table 1. Record
IdentifierMLC-T-ONC-010078
FieldOncology and biomedicine
SynonymsAR inhibitor ONCT-534; DAARI ONCT-534; dual-action androgen receptor inhibitor ONCT-534
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-010078",
  "term": "androgen receptor inhibitor ONCT-534",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable dual-action androgen receptor (AR) inhibitor, with potential antineoplastic activity. Upon oral administration, AR inhibitor ONCT-534 targets and binds to both the ligand-binding domain (LBD) and the N-terminal domain (NTD) of the AR, and inhibits AR-mediated signaling and induces the degradation of AR and AR splice variant (AR-SV) proteins. This may inhibit cell growth in AR-overexpressing tumor cells, including those with AR amplification, mutations in the AR LBD, and AR-SVs with loss of the AR LBD. AR is overexpressed in prostate cancers and is involved in the proliferation, survival and chemoresistance of tumor cells.",
  "synonyms": [
    "AR inhibitor ONCT-534",
    "DAARI ONCT-534",
    "dual-action androgen receptor inhibitor ONCT-534"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/androgen-receptor-inhibitor-onct-534/"
}

Record 1,087 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.