Preferred Label : BRD4 Protein Degrader RNK05047;
NCIt synonyms : BRD4 Degrader RNK05047; BRD4-targeting CHAMP Protein Degrader RNK05047; BRD4-targeting Protein Degrader RNK05047;
NCIt 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.;
Molecule name : RNK-05047; RNK 05047;
NCI Metathesaurus CUI : CL1798650;
Origin ID : C189823;
UMLS CUI : C5706555;
Semantic type(s)
- concept_is_in_subset
- has_target
