Preferred Label : USP1 Inhibitor SIM0501;
NCIt definition : An orally bioavailable non-covalent small molecule inhibitor of the human deubiquitinating
enzyme ubiquitin specific protease 1 (USP1; ubiquitin carboxyl-terminal hydrolase
1), with potential antineoplastic activity. Upon oral administration, USP1 inhibitor
SIM0501 specifically targets, binds to and inhibits the activity of USP1, thereby
blocking complex formation of USP1 with USP1-associated factor 1 (UAF1), and inhibits
USP1-mediated deubiquitinating activity. This may result in replication fork degradation,
accumulation of mono-ubiquinated substrates, inhibition of DNA damage repair, induction
of cell cycle arrest and apoptosis, and decreased survival of susceptible tumor cells.
USP1, overexpressed in various tumor cell types, plays a key role in the correct folding
and deubiquitylation of proteins and facilitates DNA repair via its role in regulating
the Fanconi anemia complex and translesion synthesis. It plays an important role in
the proliferation and survival of homologous repair deficiency (HRD)-positive tumor
cells.;
Molecule name : SIM 0501; SIM-0501;
Origin ID : C212940;
concept_is_in_subset
- has_target
