Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
oleh: Jennifer Cantley, Xiaofen Ye, Emma Rousseau, Tom Januario, Brian D. Hamman, Christopher M. Rose, Tommy K. Cheung, Trent Hinkle, Leofal Soto, Connor Quinn, Alicia Harbin, Elizabeth Bortolon, Xin Chen, Roy Haskell, Eva Lin, Shang-Fan Yu, Geoff Del Rosario, Emily Chan, Debra Dunlap, Hartmut Koeppen, Scott Martin, Mark Merchant, Matt Grimmer, Fabio Broccatelli, Jing Wang, Jennifer Pizzano, Peter S. Dragovich, Michael Berlin, Robert L. Yauch
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2022-11-01 |
Deskripsi
SMARCA2 has been identified as a synthetic lethal target in SMARCA4 mutated tumors, however, homology between the two has hindered the development of selective SMARCA2 inhibitors. Here, the authors synthesize a proteolysis targeting chimera (PROTAC) capable of SMARCA2 specific degradation and demonstrate its utility in the treatment of SMARCA4 mutated tumors.