selective human estrogen-receptor alpha partial agonist TTC-352

{
  "id": "MLC-T-ONC-016673",
  "term": "selective human estrogen-receptor alpha partial agonist TTC-352",
  "field": "Oncology and biomedicine",
  "definition": "A benzothiophene and orally bioavailable selective human estrogen receptor alpha (ERalpha; ESR1; ERa) partial agonist (ShERPA), with potential antineoplastic activity. Upon administration, TTC-352 mimics the naturally-occurring 17beta-estradiol (E2) and targets and binds to ERa located in the nucleus. This causes translocation of ERa to extranuclear sites. Nuclear export of ERa prevents normal ER-mediated signaling and inhibits proliferation of ER-positive tumor cells. TTC-352 causes tumor regression of tamoxifen (TAM)-resistant (TR) tumor cells which often overexpress protein kinase C alpha (PKCalpha; PKCa). PKCa expression is associated with poor patient survival and breast cancer aggressiveness and may predict tumor responses to E2, E2-like compounds and ShERPAs. Unlike E2 and E2-like compounds, TTC-352 does not cause endometrial proliferation.",
  "synonyms": [
    "ERa partial agonist TTC-352",
    "selective estrogen mimic TTC-352",
    "selective estrogen modulator TTC-352",
    "SEM TTC-352",
    "ShERPA TTC-352"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/selective-human-estrogen-receptor-alpha-partial-agonist-ttc-352/"
}