Discovery of Potent and Selective Antibody–Drug Conjugates with Eg5 Inhibitors through Linker and Payload Optimization

[Image: see text] Targeted antimitotic agents are a promising class of anticancer therapies. Herein, we describe the development of a potent and selective antimitotic Eg5 inhibitor based antibody–drug conjugate (ADC). Preliminary studies were performed using proprietary Eg5 inhibitors which were con...

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Published in:ACS Med Chem Lett
Main Authors: Karpov, Alexei S., Nieto-Oberhuber, Cristina M., Abrams, Tinya, Beng-Louka, Edwige, Blanco, Enrique, Chamoin, Sylvie, Chene, Patrick, Dacquignies, Isabelle, Daniel, Dylan, Dillon, Michael P., Doumampouom-Metoul, Lionel, Drosos, Nikolaos, Fedoseev, Pavel, Furegati, Markus, Granda, Brian, Grotzfeld, Robert M., Hess Clark, Suzanna, Joly, Emilie, Jones, Darryl, Lacaud-Baumlin, Marion, Lagasse-Guerro, Stephanie, Lorenzana, Edward G., Mallet, William, Martyniuk, Piotr, Marzinzik, Andreas L., Mesrouze, Yannick, Nocito, Sandro, Oei, Yoko, Perruccio, Francesca, Piizzi, Grazia, Richard, Etienne, Rudewicz, Patrick J., Schindler, Patrick, Velay, Mélanie, Venstrom, Kristine, Wang, Peiyin, Zurini, Mauro, Lafrance, Marc
Format: Artigo
Language:Inglês
Published: American Chemical Society 2019
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC6912867/
https://ncbi.nlm.nih.gov/pubmed/31857845
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00468
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