Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

• Published in: Bioorganic & medicinal chemistry letters Vol. 30; no. 4; p. 126907
• Main Authors: Dragovich, Peter S., Adhikari, Pragya, Blake, Robert A., Blaquiere, Nicole, Chen, Jinhua, Cheng, Yun-Xing, den Besten, Willem, Han, Jinping, Hartman, Steven J., He, Jintang, He, Mingtao, Rei Ingalla, Ellen, Kamath, Amrita V., Kleinheinz, Tracy, Lai, Tommy, Leipold, Douglas D., Li, Chun Sing, Liu, Qi, Lu, Jiawei, Lu, Ying, Meng, Fanwei, Meng, Lingyao, Ng, Carl, Peng, Kaishan, Lewis Phillips, Gail, Pillow, Thomas H., Rowntree, Rebecca K., Sadowsky, Jack D., Sampath, Deepak, Staben, Leanna, Staben, Steven T., Wai, John, Wan, Kunpeng, Wang, Xinxin, Wei, BinQing, Wertz, Ingrid E., Xin, Jianfeng, Xu, Keyang, Yao, Hui, Zang, Richard, Zhang, Donglu, Zhou, Hao, Zhao, Yongxin
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15.02.2020
• Subjects: Antibodies, Monoclonal - chemistry; Antibodies, Monoclonal - immunology; Antibody-drug conjugates; Antineoplastic Agents - chemistry; Antineoplastic Agents - immunology; Antineoplastic Agents - pharmacology; Chimeric protein degraders; Drug Carriers - chemistry; Drug delivery; Drug Design; Estrogen receptor; Estrogen Receptor alpha - immunology; Estrogen Receptor alpha - metabolism; Humans; Immunoconjugates - chemistry; Immunoconjugates - immunology; Immunoconjugates - pharmacology; MCF-7 Cells; Proteolysis - drug effects; Receptor, ErbB-2 - metabolism; Estrogen receptor; Drug delivery; Chimeric protein degraders; Antibody-drug conjugates

[Display omitted] Chimeric molecules which effect intracellular degradation of target proteins via E3 ligase-mediated ubiquitination (e.g., PROTACs) are currently of high interest in medicinal chemistry. However, these entities are relatively large compounds that often possess molecular characterist...