BRD4 protein degrader RNK05047
Term · Oncology and biomedicine · MLC-T-ONC-012106
A small molecule, chaperone-mediated protein degrader of bromodomain-containing protein 4 (BRD4), with potential antineoplastic activity. Upon intravenous administration of BRD4 protein degrader RNK05047, a BRD4-binding moiety targets and binds to BRD4, and a chaperone-binding moiety targets and binds to the chaperone protein heat shock protein 90 (Hsp90). This results in the Hsp90-mediated proteasomal degradation of BRD4 by the ubiquitin-proteasome system, and dysregulates gene expression. This may lead to the downregulation of the expression of certain growth-promoting genes, which may induce apoptosis and inhibit the proliferation of BRD4-overexpressing tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins, is a transcriptional regulator that is overexpressed in certain tumor cells and plays an important role in cellular proliferation. Hsp90 is upregulated in a variety of tumor cells and regulates the folding, stability, and degradation of many oncogenic signaling proteins.
| Identifier | MLC-T-ONC-012106 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | BRD4-targeting protein degrader RNK05047; BRD4 degrader RNK05047; BRD4-targeting CHAMP protein degrader RNK05047 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-012106",
"term": "BRD4 protein degrader RNK05047",
"field": "Oncology and biomedicine",
"definition": "A small molecule, chaperone-mediated protein degrader of bromodomain-containing protein 4 (BRD4), with potential antineoplastic activity. Upon intravenous administration of BRD4 protein degrader RNK05047, a BRD4-binding moiety targets and binds to BRD4, and a chaperone-binding moiety targets and binds to the chaperone protein heat shock protein 90 (Hsp90). This results in the Hsp90-mediated proteasomal degradation of BRD4 by the ubiquitin-proteasome system, and dysregulates gene expression. This may lead to the downregulation of the expression of certain growth-promoting genes, which may induce apoptosis and inhibit the proliferation of BRD4-overexpressing tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins, is a transcriptional regulator that is overexpressed in certain tumor cells and plays an important role in cellular proliferation. Hsp90 is upregulated in a variety of tumor cells and regulates the folding, stability, and degradation of many oncogenic signaling proteins.",
"synonyms": [
"BRD4-targeting protein degrader RNK05047",
"BRD4 degrader RNK05047",
"BRD4-targeting CHAMP protein degrader RNK05047"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/brd4-protein-degrader-rnk05047/"
}
Record 3,818 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.