PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models

Author:

Berlin Michael1,Cantley Jennifer1,Bookbinder Mark1,Bortolon Elizabeth1,Broccatelli Fabio2,Cadelina Greg1,Chan Emily W.2,Chen Huifen2ORCID,Chen Xin1,Cheng Yunxing3,Cheung Tommy K.2,Davenport Kim1,DiNicola Dean1,Gordon Debbie1,Hamman Brian D.1,Harbin Alicia1,Haskell Roy1,He Mingtao3,Hole Alison J.4,Januario Thomas2,Kerry Philip S.4,Koenig Stefan G.2ORCID,Li Limei3,Merchant Mark2,Pérez-Dorado Inmaculada4,Pizzano Jennifer1,Quinn Connor1,Rose Christopher M.2ORCID,Rousseau Emma1,Soto Leofal1,Staben Leanna R.2,Sun Hongming3,Tian Qingping2,Wang Jing1,Wang Weifeng3,Ye Crystal S.2,Ye Xiaofen2,Zhang Penghong3,Zhou Yuhui2,Yauch Robert2,Dragovich Peter S.2ORCID

Affiliation:

1. Arvinas LLC, 5 Science Park, New Haven, Connecticut 06511, United States

2. Genentech Inc., 1 DNA Way, South San Francisco, California 94080, United States

3. Pharmaron Beijing, Co. Ltd., 6 Tai He Road, BDA, Beijing 100176, P. R. China

4. Evotec (U.K.) Ltd., 95 Park Drive, Milton Park, Abingdon, Oxfordshire OX14 4RY, U.K.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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