Gintemetostat

{
  "id": "MLC-T-ONC-013946",
  "term": "Gintemetostat",
  "field": "Oncology and biomedicine",
  "definition": "An orally available small molecule inhibitor of the histone-lysine N-methyltransferase nuclear receptor-binding SET domain protein 2 (NSD2; MMSET; WHSC1), with potential antineoplastic activity. Upon oral administration, gintemetostat selectively targets and binds to NSD2, and inhibits its catalytic activity and the mono- and di-methylation of histone H3 lysine 36 (H3K36). This modulates the expression of genes involved in cellular processes including cellular proliferation, which may lead to decreased growth of cancer cells. NSD2, a member of the NSD family of histone lysine methyltransferase enzymes that catalyzes the mono- and di-methylation of H3K36, is overexpressed and dysregulated in many types of cancers.",
  "synonyms": [
    "MMSET inhibitor KTX-1001",
    "WHSC1 inhibitor KTX-1001",
    "NSD2 Inhibitor KTX-1001"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/gintemetostat/"
}