USP1 inhibitor KSQ-4279
Term · Oncology and biomedicine · MLC-T-ONC-017428
An orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1), with apoptosis-inducing, tumor-sensitizing and antineoplastic activities. Upon oral administration, USP1 inhibitor KSQ-4279 specifically binds to and inhibits the activity of USP1, thereby blocking USP1-mediated deubiquitylating activity. This blocks the ubiquitin proteasome degradation pathway, prevents the degradation of defective proteins, and leads to an accumulation of mono-ubiquinated substrates. This induces the unfolded protein response (UPR). This may induce cell cycle arrest, reduce the expression of certain anti-apoptotic proteins, induce tumor cell apoptosis, inhibit tumor cell growth, and may sensitize tumor cells to DNA-targeting chemotherapeutics. USP1, a deubiquitinating enzyme overexpressed in various tumor cell types, plays a key role in the correct folding and deubiquitination of proteins and facilitates DNA repair via its role regulating the Fanconi anemia complex and translesion synthesis.
| Identifier | MLC-T-ONC-017428 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | ubiquitin specific protease 1 inhibitor KSQ-4279 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-017428",
"term": "USP1 inhibitor KSQ-4279",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1), with apoptosis-inducing, tumor-sensitizing and antineoplastic activities. Upon oral administration, USP1 inhibitor KSQ-4279 specifically binds to and inhibits the activity of USP1, thereby blocking USP1-mediated deubiquitylating activity. This blocks the ubiquitin proteasome degradation pathway, prevents the degradation of defective proteins, and leads to an accumulation of mono-ubiquinated substrates. This induces the unfolded protein response (UPR). This may induce cell cycle arrest, reduce the expression of certain anti-apoptotic proteins, induce tumor cell apoptosis, inhibit tumor cell growth, and may sensitize tumor cells to DNA-targeting chemotherapeutics. USP1, a deubiquitinating enzyme overexpressed in various tumor cell types, plays a key role in the correct folding and deubiquitination of proteins and facilitates DNA repair via its role regulating the Fanconi anemia complex and translesion synthesis.",
"synonyms": [
"ubiquitin specific protease 1 inhibitor KSQ-4279"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/usp1-inhibitor-ksq-4279/"
}
Record 17,022 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.