ganetespib
Term · Oncology and biomedicine · MLC-T-ONC-003402
A substance being studied in the treatment of some types of cancer. Ganetespib blocks the activity of a protein called HSP90. This prevents the breakdown of certain proteins inside cells. Blocking the activity of this protein in cancer cells may help keep the cells from dividing and cause them to die. It may also make cancer cells easier to kill with chemotherapy and radiation therapy. Ganetespib is a type of heat-shock protein inhibitor.
A synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Ganetespib binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition.
| Identifier | MLC-T-ONC-003402 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | Hsp90 inhibitor STA-9090 |
| References | NCI Dictionary of Cancer Terms; National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-003402",
"term": "ganetespib",
"field": "Oncology and biomedicine",
"definitions": [
"A substance being studied in the treatment of some types of cancer. Ganetespib blocks the activity of a protein called HSP90. This prevents the breakdown of certain proteins inside cells. Blocking the activity of this protein in cancer cells may help keep the cells from dividing and cause them to die. It may also make cancer cells easier to kill with chemotherapy and radiation therapy. Ganetespib is a type of heat-shock protein inhibitor.",
"A synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Ganetespib binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of \"client\" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition."
],
"synonyms": [
"Hsp90 inhibitor STA-9090"
],
"references": [
"NCI Dictionary of Cancer Terms",
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/ganetespib/"
}
Record 7,793 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.