Novel WRN Helicase Inhibitors Selectively Target Microsatellite Unstable Cancer Cells.
Picco G, Rao Y, Al Saedi A, Lee Y, Vieira SF, Bhosle S, May K, Herranz-Ors C, Walker SJ, Shenje R, Dincer C, Gibson F, Banerjee R, Hewitson Z, Werner T, Cottom JE, Peng Y, Deng N, Landis P, Conticelli D, McCarten K, Bush J, Sharma M, Lightfoot H, House D, Milford E, Grant EK, Glogowski MP, Wagner CD, Bantscheff M, Rutkowska-Klute A, Network Uk Group CM, Zappacosta F, Pettinger J, Barthorpe S, Eberl HC, Jones BT, Schneck JL, Murphy DJ, Voest EE, Taygerly JP, DeMartino MP, Coelho MA, Houseley J, Sharma G, Schwartz BJ, Garnett MJ.
Picco G, et al.
Cancer Discov. 2024 Apr 9. doi: 10.1158/2159-8290.CD-24-0052. Online ahead of print.
Cancer Discov. 2024.
PMID: 38587317
Microsatellite-unstable (MSI) cancers require WRN helicase to resolve replication stress due to expanded DNA (TA)n-dinucleotide repeats. WRN is a promising synthetic lethal target for MSI tumours, and WRN inhibitors are in development. ...Fragment-based screening led to th …
Microsatellite-unstable (MSI) cancers require WRN helicase to resolve replication stress due to expanded DNA (TA)n-dinucleotide repea …