MLchartDataset catalogue

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.

Table 1. Record
IdentifierMLC-T-ONC-017428
FieldOncology and biomedicine
Synonymsubiquitin specific protease 1 inhibitor KSQ-4279
ReferencesNational 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.