Preferred Label : WRN Inhibitor HRO761;
NCIt synonyms : WRN Helicase Inhibitor HRO761; Werner Syndrome RecQ DNA Helicase Inhibitor HRO761;
NCIt definition : An orally bioavailable selective and allosteric inhibitor of the Werner syndrome ATP-dependent
helicase (WRN), with potential antineoplastic activity. Upon oral administration,
WRN inhibitor HRO761 allosterically binds at the interface of the D1 and D2 helicase
domains of WRN, thereby locking WRN in an inactive conformation. This induces double-stranded
DNA breaks and activates the DNA damage response (DDR) to induce WRN degradation.
This promotes cell cycle arrest and cell death in, and inhibits the growth of susceptible
tumor cells, such as ones with high microsatellite instability (MSI-H). WRN, a multifunctional
enzyme with both helicase and exonuclease activities, plays a key role in DNA replication
and repair. It is overexpressed in a variety of cancer cells.;
Molecule name : HRO 761; HRO-761;
Origin ID : C210827;
concept_is_in_subset
- has_target
