Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers.

doi:10.1038/s41467-022-34562-5

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Article

Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers.

Nature communications - 10 Nov 2022

Cantley Jennifer, Ye Xiaofen, Rousseau Emma, Januario Tom, Hamman Brian D, Rose Christopher M, Cheung Tommy K, Hinkle Trent, Soto Leofal, Quinn Connor, Harbin Alicia, Bortolon Elizabeth, Chen Xin, Haskell Roy, Lin Eva, Yu Shang-Fan, Del Rosario Geoff, Chan Emily, Dunlap Debra, Koeppen Hartmut, Martin Scott, Merchant Mark, Grimmer Matt, Broccatelli Fabio, Wang Jing, Pizzano Jennifer, Dragovich Peter S, Berlin Michael, Yauch Robert L

Abstract excerpt

The mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4 is frequently mutated in cancer and inactivation results in a cellular dependence on its paralog, SMARCA2, thus making SMARCA2 an attractive synthetic lethal target. However, published data indicates that achieving a high degree of selective SMARCA2 inhibition is likely essential to afford an acceptable therapeutic index, and realizing this...

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PMID: 36357397
DOI: 10.1038/s41467-022-34562-5
PMCID: PMC9649729

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