MLchartDataset catalogue

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.

Table 1. Record
IdentifierMLC-T-ONC-013895
FieldOncology and biomedicine
AbbreviationG-TPP
Synonymsgamitrinib-TPP
ReferencesNational 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.