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Application: Screen small molecule inhibitors or antagonists that affect helicase activity of WRN in high throughput screening (HTS) applications.
Background: The WRN gene was first discovered as the gene mutated in Werner syndrome, a recessive genetic disorder characterized by segmental progeria and elevated cancer predisposition. WRN is a multifunctional enzyme with helicase and exonuclease activities and plays roles in various cellular processes crucial for the maintenance of genome stability, including DNA replication, transcription, DNA repair, and telomere maintenance. WRN depletion causes cell cycle arrest, DNA damage, mitotic defects, chromosome shattering, and apoptosis. Loss of heterozygosity involving the WRN loci at chromosome 8p11.2-p12 occurs frequently in many different cancers, pointing to its role as a tumor suppressor gene. Small molecule inhibitors of WRN can be used to induce synthetic lethality and offer a new therapeutical approach for cancer treatment.
Contraindications: The final concentration of DMSO in the reaction should not exceed 1%.
Description: The WRN ATPase Activity Assay Kit is designed for screening and profiling of WRN (Werner Syndrome ATP-dependent Helicase) antagonists/inhibitors by monitoring their effect on the conversion of ATP to ADP using ADP-Glo™ as a detection reagent. ATP conversion to ADP occurs during DNA unwinding by the ATP dependent helicase domain of WRN. WRN ATPase Activity Assay Kit comes in a convenient 96-well format, with enough purified recombinant WRN (amino acids 517-1093), ATP, WRN substrate, assay buffer and additives for 100 reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Target: WRN
Uniprot: Q14191
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Mendoza, O., et al. 2015. Nucleic Acids Res 43(11): e71.Van Wietmarschen, N., et al. 2021. Curr Opin Genet Dev 71: 34-38.
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