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.
| Identifier | MLC-T-ONC-014312 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | IDH2 R140Q mutant inhibitor SH1573; mIDH2 inhibitor SH1573 |
| References | National 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.