MLchartDataset catalogue

BCL6 degrader ARV-393

Term · Oncology and biomedicine · MLC-T-ONC-011908

An orally bioavailable, targeted degrader composed of an E3 ubiquitin ligase-binding moiety that is conjugated, via a linker, to a B-cell lymphoma 6 protein (BCL6; BCL-6)-binding moiety using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Upon oral administration of BCL6 degrader ARV-393, the BCL6-binding moiety specifically targets and binds to BCL6 on tumor cells while the E3 ubiquitin ligase-binding moiety targets and binds to E3 ubiquitin ligase, thereby creating a ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation of BCL6. This prevents BCL6-mediated signaling and activation of downstream survival pathways. This leads to an inhibition of the growth of tumor cells that overexpress BCL6. BCL6, a transcriptional repressor overexpressed in certain tumor cells, serves an important role in cell signaling and tumor cell proliferation.

Table 1. Record
IdentifierMLC-T-ONC-011908
FieldOncology and biomedicine
SynonymsPROTAC BCL6 degrader ARV-393; proteolysis-targeting chimera protein degrader ARV-393
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-011908",
  "term": "BCL6 degrader ARV-393",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, targeted degrader composed of an E3 ubiquitin ligase-binding moiety that is conjugated, via a linker, to a B-cell lymphoma 6 protein (BCL6; BCL-6)-binding moiety using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Upon oral administration of BCL6 degrader ARV-393, the BCL6-binding moiety specifically targets and binds to BCL6 on tumor cells while the E3 ubiquitin ligase-binding moiety targets and binds to E3 ubiquitin ligase, thereby creating a ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation of BCL6. This prevents BCL6-mediated signaling and activation of downstream survival pathways. This leads to an inhibition of the growth of tumor cells that overexpress BCL6. BCL6, a transcriptional repressor overexpressed in certain tumor cells, serves an important role in cell signaling and tumor cell proliferation.",
  "synonyms": [
    "PROTAC BCL6 degrader ARV-393",
    "proteolysis-targeting chimera protein degrader ARV-393"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/bcl6-degrader-arv-393/"
}

Record 3,352 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.