Gamitrinib
Term · Oncology and biomedicine · MLC-T-ONC-013895
A resorcinolic-based mitochondrial-targeted heat shock protein 90 (Hsp90) family inhibitor, with potential antineoplastic activity. Upon administration, gamitrinib targets and inhibits the activity of Hsp90 heat shock proteins, such as TNF receptor-associated protein-1 (TRAP1). This induces the accumulation of the mitochondrial kinase PINK1 and the cytosolic E3 ubiquitin (Ub) ligase Parkin, ubiquitylates substrate proteins, and induces PINK1/Parkin-dependent mitophagy. Gamitrinib induces acute mitochondrial dysfunction, loss of membrane potential and membrane rupture leading to the induction of apoptosis in susceptible tumor cells. Hsp90, a chaperone complex protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins.
| Identifier | MLC-T-ONC-013895 |
|---|---|
| Field | Oncology and biomedicine |
| Abbreviation | G-TPP |
| Synonyms | gamitrinib-TPP |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-013895",
"term": "Gamitrinib",
"field": "Oncology and biomedicine",
"definition": "A resorcinolic-based mitochondrial-targeted heat shock protein 90 (Hsp90) family inhibitor, with potential antineoplastic activity. Upon administration, gamitrinib targets and inhibits the activity of Hsp90 heat shock proteins, such as TNF receptor-associated protein-1 (TRAP1). This induces the accumulation of the mitochondrial kinase PINK1 and the cytosolic E3 ubiquitin (Ub) ligase Parkin, ubiquitylates substrate proteins, and induces PINK1/Parkin-dependent mitophagy. Gamitrinib induces acute mitochondrial dysfunction, loss of membrane potential and membrane rupture leading to the induction of apoptosis in susceptible tumor cells. Hsp90, a chaperone complex protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins.",
"abbreviation": "G-TPP",
"synonyms": [
"gamitrinib-TPP"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/gamitrinib/"
}
Record 7,780 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.