p97 Inhibitor CB-5339
Term · Oncology and biomedicine · MLC-T-ONC-015758
An orally bioavailable, selective, second-generation inhibitor of valosin-containing protein (VCP)/p97, with potential antineoplastic activity. Upon oral administration, p97 inhibitor CB-5339 binds to and inhibits the activity of p97. This prevents ubiquitin-dependent protein degradation and causes cellular accumulation of poly-ubiquitinated proteins. The inhibition of endoplasmic reticulum (ER)-associated protein degradation activates the ER-dependent stress response pathway, and leads to both an induction of apoptosis and the inhibition of cell proliferation in susceptible tumor cells. VCP/p97, a type II AAA+ ATPase, plays a key role in cellular protein homeostasis processes including ER-associated degradation (ERAD), chromatin associated degradation (CAD) and the DNA damage response (DDR). Its overexpression in many tumor cell types is associated with increased tumor cell proliferation and survival.
| Identifier | MLC-T-ONC-015758 |
|---|---|
| Field | Oncology and biomedicine |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-015758",
"term": "p97 Inhibitor CB-5339",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable, selective, second-generation inhibitor of valosin-containing protein (VCP)/p97, with potential antineoplastic activity. Upon oral administration, p97 inhibitor CB-5339 binds to and inhibits the activity of p97. This prevents ubiquitin-dependent protein degradation and causes cellular accumulation of poly-ubiquitinated proteins. The inhibition of endoplasmic reticulum (ER)-associated protein degradation activates the ER-dependent stress response pathway, and leads to both an induction of apoptosis and the inhibition of cell proliferation in susceptible tumor cells. VCP/p97, a type II AAA+ ATPase, plays a key role in cellular protein homeostasis processes including ER-associated degradation (ERAD), chromatin associated degradation (CAD) and the DNA damage response (DDR). Its overexpression in many tumor cell types is associated with increased tumor cell proliferation and survival.",
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/p97-inhibitor-cb-5339/"
}
Record 12,481 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.