selective estrogen receptor covalent antagonist H3B-6545

{
  "id": "MLC-T-ONC-016666",
  "term": "selective estrogen receptor covalent antagonist H3B-6545",
  "field": "Oncology and biomedicine",
  "definition": "An orally available, selective and covalent antagonist of estrogen receptor alpha (ERalpha; ERa; ESR1; nuclear receptor subfamily 3, group A, member 1; NR3A1), with potential antineoplastic activity. Upon oral administration, selective estrogen receptor covalent antagonist (SERCA) H3B-6545 selectively and covalently binds to a cysteine that is unique to ERalpha and is not present in other nuclear hormone receptors, thereby inhibiting the activity of ERalpha. This inhibits the growth and survival of ERalpha-expressing cancer cells. ERalpha, a nuclear hormone receptor, is often overexpressed and/or mutated in a variety of cancer cell types. It plays a key role in tumor cell proliferation and survival.",
  "synonyms": [
    "SERCA H3B-6545"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/selective-estrogen-receptor-covalent-antagonist-h3b-6545/"
}