MLchartDataset catalogue

IDH2 mutant inhibitor SH1573

Term · Oncology and biomedicine · MLC-T-ONC-014312

An orally bioavailable inhibitor of mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2; IDH-2) R140Q mutant, with potential antineoplastic activity. Upon oral administration, IDH2 mutant inhibitor SH1573 specifically inhibits mutant IDH2 (mIDH2) R140Q protein, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing mIDH2 R140Q. IDH2 is mutated in a variety of cancers, and mutated IDH2 initiates and drives cancer growth by catalyzing the formation of 2HG and blocking cell differentiation.

Table 1. Record
IdentifierMLC-T-ONC-014312
FieldOncology and biomedicine
SynonymsIDH2 R140Q mutant inhibitor SH1573; mIDH2 inhibitor SH1573
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-014312",
  "term": "IDH2 mutant inhibitor SH1573",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable inhibitor of mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2; IDH-2) R140Q mutant, with potential antineoplastic activity. Upon oral administration, IDH2 mutant inhibitor SH1573 specifically inhibits mutant IDH2 (mIDH2) R140Q protein, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing mIDH2 R140Q. IDH2 is mutated in a variety of cancers, and mutated IDH2 initiates and drives cancer growth by catalyzing the formation of 2HG and blocking cell differentiation.",
  "synonyms": [
    "IDH2 R140Q mutant inhibitor SH1573",
    "mIDH2 inhibitor SH1573"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/idh2-mutant-inhibitor-sh1573/"
}

Record 8,929 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.