Nature Communications (Nov 2022)
Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
- 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
Affiliations
- Jennifer Cantley
- Arvinas, LLC
- Xiaofen Ye
- Genentech
- Emma Rousseau
- Arvinas, LLC
- Tom Januario
- Genentech
- Brian D. Hamman
- HotSpot Therapeutics
- Christopher M. Rose
- Genentech
- Tommy K. Cheung
- Genentech
- Trent Hinkle
- Genentech
- Leofal Soto
- Arvinas, LLC
- Connor Quinn
- Arvinas, LLC
- Alicia Harbin
- Arvinas, LLC
- Elizabeth Bortolon
- Arvinas, LLC
- Xin Chen
- Arvinas, LLC
- Roy Haskell
- Arvinas, LLC
- Eva Lin
- Genentech
- Shang-Fan Yu
- Genentech
- Geoff Del Rosario
- Genentech
- Emily Chan
- Genentech
- Debra Dunlap
- Genentech
- Hartmut Koeppen
- Genentech
- Scott Martin
- Genentech
- Mark Merchant
- Genentech
- Matt Grimmer
- Genentech
- Fabio Broccatelli
- Genentech
- Jing Wang
- Arvinas, LLC
- Jennifer Pizzano
- Arvinas, LLC
- Peter S. Dragovich
- Genentech
- Michael Berlin
- Arvinas, LLC
- Robert L. Yauch
- Genentech
- DOI
- https://doi.org/10.1038/s41467-022-34562-5
- Journal volume & issue
-
Vol. 13,
no. 1
pp. 1 – 14
Abstract
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.
