p300/CBP bromodomain inhibitor CCS1477

{
  "id": "MLC-T-ONC-015744",
  "term": "p300/CBP bromodomain inhibitor CCS1477",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, small molecule inhibitor of the highly conserved bromodomains of the histone acetyltransferase (HAT) paralogs, p300 (E1A-associated protein p300; p300 HAT) and CREB binding protein (CBP), with potential antineoplastic activity. Upon oral administration, p300/CBP bromodomain inhibitor CCS1477 selectively and reversibly binds to the bromodomains of p300 and CBP. This disrupts the acetylation of histones and other proteins and prevents the co-activation of key transcription factors that contribute to tumor progression including the androgen receptor (AR), androgen receptor splice variants (AR-SV), hypoxia-inducible factor 1-alpha (HIF-1-alpha) and Myc proto-oncogene protein (c-Myc). The HAT paralogs p300 and CBP are key transcriptional co-activators that are essential for a multitude of cellular processes and are implicated in the progression and therapeutic resistance of certain cancers.",
  "synonyms": [
    "p300 HAT/CREB binding protein inhibitor CCS1477"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/p300-cbp-bromodomain-inhibitor-ccs1477/"
}