Preferred Label : USP1 inhibitor KSQ-4279;
NCIt synonyms : Ubiquitin Specific Protease 1 Inhibitor KSQ-4279;
NCIt related terms : KSQ-4279;
NCIt 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.;
UNII : HK5F3RGM8P;
Molecule name : KSQ-4279; KSQ 4279;
NCI Metathesaurus CUI : CL1773874;
Origin ID : C185613;
UMLS CUI : C5667018;
Semantic type(s)
- concept_is_in_subset
- has_target
