PI3K-alpha inhibitor JS105
Term · Oncology and biomedicine · MLC-T-ONC-016038
An orally bioavailable inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA), with potential antineoplastic activity. Upon oral administration, PI3K-alpha inhibitor JS105 selectively targets, binds to and inhibits PIK3CA in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting PIK3CA, JS105 may be more efficacious and less toxic than pan-PI3K inhibitors. Dysregulation of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA, one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K.
| Identifier | MLC-T-ONC-016038 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | PI3K alpha inhibitor JS105; PI3K-a inhibitor JS105 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-016038",
"term": "PI3K-alpha inhibitor JS105",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA), with potential antineoplastic activity. Upon oral administration, PI3K-alpha inhibitor JS105 selectively targets, binds to and inhibits PIK3CA in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting PIK3CA, JS105 may be more efficacious and less toxic than pan-PI3K inhibitors. Dysregulation of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA, one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K.",
"synonyms": [
"PI3K alpha inhibitor JS105",
"PI3K-a inhibitor JS105"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/pi3k-alpha-inhibitor-js105/"
}
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