PPAR gamma inhibitor FX-909

{
  "id": "MLC-T-ONC-016198",
  "term": "PPAR gamma inhibitor FX-909",
  "field": "Oncology and biomedicine",
  "definition": "An orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator-activated receptor gamma (PPAR gamma; PPARG), with potential antineoplastic activity. Upon oral administration, PPARG inhibitor FX-909 selectively targets and covalently binds to a region of PPARG that is sequestered from the mutation site. The binding promotes a repressive conformation of PPARG and inhibits the activity of PPARG. This inhibits both basal- and ligand-activated transcription by PPARG and prevents PPARG-mediated transcription of target genes, such as FABP4/Fabp4, AGT/Agt, IVT/Ivd and ARG1/Arg1. This may inhibit proliferation in PPARG-overactivated tumor cells. PPARG, a nuclear receptor, is genetically altered, including amplification, missense mutations, and fusions, in certain tumor cells commonly associated with the luminal lineage subtype.",
  "synonyms": [
    "peroxisome proliferator-activated receptor gamma inhibitor FX-909",
    "PPAR-gamma inhibitor FX-909",
    "PPARG inhibitor FX-909",
    "PPARG inverse agonist FX-909"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/ppar-gamma-inhibitor-fx-909/"
}