estrogen receptor degrader AC699
Term · Oncology and biomedicine · MLC-T-ONC-013442
An orally bioavailable estrogen receptor (ER)-targeted chimeric protein degrader composed of ligands of ER and cereblon (CRBN) E3 ubiquitin ligase, with potential antineoplastic activity. Upon oral administration of ER degrader AC699, the ER-targeting moiety targets and binds to ER, and the CRBN-binding moiety recruits CRBN, a component of the CRL4-CRBN E3 ubiquitin ligase complex. This catalyzes ubiquitination and proteasome-mediated degradation of ER, prevents ER-mediated signaling, and inhibits both the growth and survival of ER-expressing cancer cells. ER is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation.
| Identifier | MLC-T-ONC-013442 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | ER degrader AC699; ER-targeting chimeric protein degrader AC699 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-013442",
"term": "estrogen receptor degrader AC699",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable estrogen receptor (ER)-targeted chimeric protein degrader composed of ligands of ER and cereblon (CRBN) E3 ubiquitin ligase, with potential antineoplastic activity. Upon oral administration of ER degrader AC699, the ER-targeting moiety targets and binds to ER, and the CRBN-binding moiety recruits CRBN, a component of the CRL4-CRBN E3 ubiquitin ligase complex. This catalyzes ubiquitination and proteasome-mediated degradation of ER, prevents ER-mediated signaling, and inhibits both the growth and survival of ER-expressing cancer cells. ER is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation.",
"synonyms": [
"ER degrader AC699",
"ER-targeting chimeric protein degrader AC699"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/estrogen-receptor-degrader-ac699/"
}
Record 6,936 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.