CRL4-CRBN modulator KPG-818

{
  "id": "MLC-T-ONC-012810",
  "term": "CRL4-CRBN modulator KPG-818",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable modulator of the E3 ubiquitin ligase complex containing cereblon (CRL4-CRBN E3 ubiquitin ligase), with potential immunomodulating and antineoplastic activities. Upon oral administration, CRL4-CRBN modulator KPG-818 specifically targets and binds to cereblon (CRBN) of the E3 ubiquitin ligase (CRL4-CRBN) complex, thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces proteasome-mediated degradation of certain transcription factors, some of which are transcriptional repressors in T cells. This leads to modulation of the immune system, including activation of T lymphocytes, and downregulation of the activity of other proteins, some of which play key roles in the proliferation of certain cancer cell types. CRBN, the substrate recognition component of the CRL4-CRBN E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins.",
  "synonyms": [
    "cereblon E3 ubiquitin ligase modulating agent KPG-818",
    "CRBN E3 ubiquitin ligase complex CRL4-CRBN modulator KPG-818"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/crl4-crbn-modulator-kpg-818/"
}