PROTACs Targeting BRM (SMARCA2) Afford Selective <i>In Vivo</i> Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models-Reference-Cited by-同舟云学术

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

Published:2024-01-05 Issue:2 Volume:67 Page:1262-1313
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Berlin Michael¹,Cantley Jennifer¹,Bookbinder Mark¹,Bortolon Elizabeth¹,Broccatelli Fabio²,Cadelina Greg¹,Chan Emily W.²,Chen Huifen²^ORCID,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.²^ORCID,Li Limei³,Merchant Mark²,Pérez-Dorado Inmaculada⁴,Pizzano Jennifer¹,Quinn Connor¹,Rose Christopher M.²^ORCID,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.²^ORCID

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)

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.3c01781

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1. Exploiting vulnerabilities of SWI/SNF chromatin remodelling complexes for cancer therapy

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