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PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models (vol 67, pg 1262, 2024) PROTACs靶向BRM（SMARCA2）可在体内实现对BRG1（SMARCA4）的选择性降解，并在BRG1突变异种移植肿瘤模型中表现出活性（vol 67, pg 1262, 2024） Berlin, Michael; Cantley, Jennifer; Bookbinder, Mark; Bortolon, Elizabeth; Broccatelli, Fabio; Cadelina, Greg; Chan, Emily W.; Chen, Huifen; Chen, Xin; Cheng, Yunxing; Cheung, Tommy K.; Crew, Andrew P.; Davenport, Kim; Dinicola, Dean; Dong, Hanqing; Gordon, Debbie; Hamman, Brian D.; Harbin, Alicia; Haskell, Roy; He, Mingtao; Hole, Alison J.; Januario, Thomas; Kerry, Philip S.; Koenig, Stefan G.; Li, Limei; Merchant, Mark; Perez-Dorado, Inmaculada; Pizzano, Jennifer; Quinn, Connor; Rose, Christopher M.; Rousseau, Emma; Snyder, Lawrence B.; Soto, Leofal; Staben, Leanna R.; Sun, Hongming; Tian, Qingping; Wang, Gan; Wang, Jing; Wang, Weifeng; Ye, Crystal S.; Ye, Xiaofen; Zhang, Penghong; Zhou, Yuhui; Yauch, Robert; Dragovich, Peter S. 分享 收藏
Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs Zhang, Donglu; Ma, Bin; Dragovich, Peter S.; Ma, Li; Chen, Shu; Chen, Eugene C.; Ye, Xiaofen; Liu, Joyce; Pizzano, Jennifer; Bortolon, Elizabeth; Chan, Emily; Zhang, Xing; Chen, Yi-Chen; Levy, Elizabeth S.; Yauch, Robert L.; Khojasteh, S. Cyrus; Hop, Cornelis E. C. A. 分享 收藏
The HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results Lewis, Gail D.; Li, Guangmin; Guo, Jun; Yu, Shang-Fan; Fields, Carter T.; Lee, Genee; Zhang, Donglu; Dragovich, Peter S.; Pillow, Thomas; Wei, Binqing; Sadowsky, Jack; Leipold, Douglas; Wilson, Tim; Kamath, Amrita; Mamounas, Michael; Lee, M. Violet; Saad, Ola; Choeurng, Voleak; Ungewickell, Alexander; Monemi, Sharareh; Crocker, Lisa; Kalinsky, Kevin; Modi, Shanu; Jung, Kyung Hae; Hamilton, Erika; LoRusso, Patricia; Krop, Ian; Schutten, Melissa M.; Commerford, Renee; Sliwkowski, Mark X.; Cho, Eunpi 分享 收藏
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models Berlin, Michael; Cantley, Jennifer; Bookbinder, Mark; Bortolon, Elizabeth; Broccatelli, Fabio; Cadelina, Greg; Chan, Emily W.; Chen, Huifen; Chen, Xin; Cheng, Yunxing; Cheung, Tommy K.; Davenport, Kim; DiNicola, Dean; Gordon, Debbie; Hamman, Brian D.; Harbin, Alicia; Haskell, Roy; He, Mingtao; Hole, Alison J.; Januario, Thomas; Kerry, Philip S.; Koenig, Stefan G.; Li, Limei; Merchant, Mark; Perez-Dorado, Inmaculada; Pizzano, Jennifer; Quinn, Connor; Rose, Christopher M.; Rousseau, Emma; Soto, Leofal; Staben, Leanna R.; Sun, Hongming; Tian, Qingping; Wang, Jing; Wang, Weifeng; Ye, Crystal S.; Ye, Xiaofen; Zhang, Penghong; Zhou, Yuhui; Yauch, Robert; Dragovich, Peter S. 分享 收藏
Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs Kou, Ponien; Levy, Elizabeth S.; Nguyen, An D.; Zhang, Donglu; Chen, Shu; Cui, Yusi; Zhang, Xing; Broccatelli, Fabio; Pizzano, Jennifer; Cantley, Jennifer; Bortolon, Elizabeth; Rousseau, Emma; Berlin, Michael; Dragovich, Peter; Sethuraman, Vijay 分享 收藏
Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors Kschonsak, Marc; Jao, Christine C.; Arthur, Christopher P.; Rohou, Alexis L.; Bergeron, Philippe; Ortwine, Daniel F.; McKerrall, Steven J.; Hackos, David H.; Deng, Lunbin; Chen, Jun; Li, Tianbo; Dragovich, Peter S.; Volgraf, Matthew; Wright, Matthew R.; Payandeh, Jian; Ciferri, Claudio; Tellis, John C. 分享 收藏
Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers 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. 分享 收藏
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Preclinical development of DHES0815A: A HER2-directed antibody-drug conjugate comprised of a reduced potency PBD dimer linked to a domain I binding HER2 antibody Phillips, Gail Lewis; Li, Guangmin; Guo, Jun; Yu, Shang-Fan; Lee, Genee; Zhang, Donglu; Dragovich, Peter; Pillow, Thomas; Wei, Binqing; Lee, M. Violet; Saad, Ola; Masih, Shab; Leipold, Douglas; Crocker, Lisa; Schutten, Melissa 分享 收藏
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Calicheamicin Antibody-Drug Conjugates with Improved Properties Vollmar, Breanna S.; Frantz, Chris; Schutten, Melissa M.; Zhong, Fiona; Rosario, Geoffrey del; Go, Mary Ann T.; Yu, Shang-Fan; Leipold, Douglas D.; Kamath, Amrita, V; Ng, Carl; Xu, Keyang; Cruz-Chuh, Josefa Dela; Kozak, Katherine R.; Chen, Jinhua; Xu, Zijin; Wai, John; Adhikari, Pragya; Erickson, Hans K.; Dragovich, Peter S.; Polson, Andrew G.; Pillow, Thomas H. 分享 收藏
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties 嵌合BRD4降解剂的抗体介导递送。第1部分: 抗体接头，有效载荷加载和有效载荷分子特性的探索 Dragovich, Peter S.; Pillow, Thomas H.; Blake, Robert A.; Sadowsky, Jack D.; Adaligil, Emel; Adhikari, Pragya; Bhakta, Sunil; Blaquiere, Nicole; Chen, Jinhua; Dela Cruz-Chuh, Josefa; Gascoigne, Karen E.; Hartman, Steven J.; He, Mingtao; Kaufman, Susan; Kleinheinz, Tracy; Kozak, Katherine R.; Liu, Liang; Liu, Liling; Liu, Qi; Lu, Ying; Meng, Fanwei; Mulvihill, Melinda M.; O'Donohue, Aimee; Rowntree, Rebecca K.; Staben, Leanna R.; Staben, Steven T.; Wai, John; Wang, Jian; Wei, BinQing; Wilson, Catherine; Xin, Jianfeng; Xu, Zijin; Yao, Hui; Zhang, Donglu; Zhang, Hongyan; Zhou, Hao; Zhu, Xiaoyu 分享 收藏
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy 嵌合BRD4降解剂的抗体介导递送。第2部分: 体外抗增殖活性和体内抗肿瘤功效的提高 Dragovich, Peter S.; Pillow, Thomas H.; Blake, Robert A.; Sadowsky, Jack D.; Adaligil, Emel; Adhikari, Pragya; Chen, Jinhua; Corr, Nicholas; Dela Cruz-Chuh, Josefa; Del Rosario, Geoffrey; Fullerton, Aaron; Hartman, Steven J.; Jiang, Fan; Kaufman, Susan; Kleinheinz, Tracy; Kozak, Katherine R.; Liu, Liling; Lu, Ying; Mulvihill, Melinda M.; Murray, Jeremy M.; O'Donohue, Aimee; Rowntree, Rebecca K.; Sawyer, William S.; Staben, Leanna R.; Wai, John; Wang, Jian; Wei, BinQing; Wei, Wentao; Xu, Zijin; Yao, Hui; Yu, Shang-Fan; Zhang, Donglu; Zhang, Hongyan; Zhang, Shenhua; Zhao, Yongxin; Zhou, Hao; Zhu, Xiaoyu 分享 收藏
An Anti-CD22-seco-CBI-Dimer Antibody-Drug Conjugate (ADC) for the Treatment of Non-Hodgkin Lymphoma That Provides a Longer Duration of Response than Auristatin-Based ADCs in Preclinical Models Yu, Shang-Fan; Lee, Donna W.; Zheng, Bing; Del Rosario, Geoffrey; Leipold, Douglas; Booler, Helen; Zhong, Fiona; Carrasco-Triguero, Montserrat; Hong, Kyu; Yan, Peter; Rowntree, Rebecca K.; Schutten, Melissa M.; Pillow, Thomas; Sadowsky, Jack D.; Dragovich, Peter S.; Polson, Andrew G. 分享 收藏
Preclinical optimization of Ly6E-targeted ADCs for increased durability and efficacy of anti-tumor response Dela Cruz Chuh, Josefa; Go, MaryAnn; Chen, Yvonne; Guo, Jun; Rafidi, Hanine; Mandikian, Danielle; Sun, Yonglian; Lin, Zhonghua; Schneider, Kellen; Zhang, Pamela; Vij, Rajesh; Sharpnack, Danielle; Chan, Pamela; de la Cruz, Cecile; Sadowsky, Jack; Seshasayee, Dhaya; Koerber, James T.; Pillow, Thomas H.; Phillips, Gail D.; Rowntree, Rebecca K.; Boswell, C. Andrew; Kozak, Katherine R.; Polson, Andrew G.; Polakis, Paul; Yu, Shang-Fan; Dragovich, Peter S.; Agard, Nicholas J. 分享 收藏
Selective, chemically-induced degradation of BRM (SMARCA2) enables in vivo efficacy in BRG1 (SMARCA4)-deficient xenograft tumor models Berlin, Michael; Cantley, Jennifer; Wang, Jing; Bookbinder, Mark; Cadelina, Gregory; Chan, Emily; Chen, Huifen; Chen, Xin; Davenport, Kim; Fernando, Tharu; Gordon, Debbie; Hamman, Brian; Haskell, Roy; Ishchenko, Alexey; Kirkpatrick, Donald S.; Maher, Jonathan; Merchant, Mark; Moffat, John; Morgan, Alicia; Nguyen, An; Pizzano, Jennifer; Quinn, Connor; Rose, Christopher M.; Rousseau, Emma; Sethuraman, Vijay; Staben, Leanna; Wilson, Catherine; Ye, Xiaofen; Broccatelli, Fabio; Yauch, Robert; Dragovich, Peter S. 分享 收藏
Systematic Variation of Pyrrolobenzodiazepine (PBD)-Dimer Payload Physicochemical Properties Impacts Efficacy and Tolerability of the Corresponding Antibody-Drug Conjugates Staben, Leanna R.; Chen, Jinhua; dela Cruz-Chuh, Josefa; del Rosario, Geoff; Go, Mary Ann; Guo, Jun; Khojasteh, S. Cyrus; Kozak, Katherine R.; Li, Guangmin; Ng, Carl; Phillips, Gail D. Lewis; Pillow, Thomas H.; Rowntree, Rebecca K.; Wai, John; Wei, BinQing; Xu, Keyang; Xu, Zijin; Yu, Shang-Fan; Zhang, Donglu; Dragovich, Peter S. 分享 收藏
Improved translation of stability for conjugated antibodies using an in vitro whole blood assay Fourie-O'Donohue, Aimee; Chu, Phillip Y.; Chuh, Josefa dela Cruz; Tchelepi, Robert; Tsai, Siao Ping; Tran, John C.; Sawyer, William S.; Su, Dian; Ng, Carl; Xu, Keyang; Yu, Shang-Fan; Pillow, Thomas H.; Sadowsky, Jack; Dragovich, Peter S.; Liu, Yichin; Kozak, Katherine R. 分享 收藏
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