MLchartDataset catalogue

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.

Table 1. Record
IdentifierMLC-T-ONC-012106
FieldOncology and biomedicine
SynonymsBRD4-targeting protein degrader RNK05047; BRD4 degrader RNK05047; BRD4-targeting CHAMP protein degrader RNK05047
ReferencesNational 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.