Challenges for the Discovery of Non‐Covalent WRN Helicase Inhibitors
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DOI: 10.1002/cmdc.202300613
Abstract: The Werner Syndrome RecQ helicase (WRN) is a synthetic lethal target of interest for the treatment of cancers with microsatellite instability (MSI). Different hit finding approaches were initially tested. The identification of WRN inhibitors proved… read more here.
Keywords: helicase inhibitors; helicase; discovery non; wrn helicase ... See more keywords
Abstract 420: On-target mutations confer resistance to WRN helicase inhibitors in Microsatellite Unstable Cancer Cells
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DOI: 10.1158/1538-7445.am2025-420
Abstract: Werner helicase inhibitors (WRNi) are in clinical development for treating patients with microsatellite-unstable (MSI) tumors characterized by defective DNA mismatch repair. Here, we investigate the impact of cancer cell evolutionary adaptation on WRN pharmacological inhibition… read more here.
Keywords: helicase inhibitors; cancer; resistance; resistance wrn ... See more keywords