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.
| Identifier | MLC-T-ONC-010078 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | AR inhibitor ONCT-534; DAARI ONCT-534; dual-action androgen receptor inhibitor ONCT-534 |
| References | National 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.