VVD-214 is a synthetic lethal allosteric inhibitor of WRN helicase. VVD-214 covalently binds to cysteine 727 of WRN and inhibits ATP drolysis and helicase activity. VVD-214 is potent in causing double-stranded DNA breaks, nuclear swelling, and cell death in high microsatellite instability (MSI) cancers.
References:
[1]. Kikuchi S, et al. Abstract ND11: Chemoproteomic-enabled discovery of VVD-214, a synthetic lethal allosteric inhibitor of WRN helicase[J]. Cancer Research, 2024, 84(7_Supplement): ND11-ND11.
















