Optimization of Tubulysin Antibody–Drug Conjugates: A Case Study in Addressing ADC Metabolism

[Image: see text] As part of our efforts to develop new classes of tubulin inhibitor payloads for antibody–drug conjugate (ADC) programs, we developed a tubulysin ADC that demonstrated excellent in vitro activity but suffered from rapid metabolism of a critical acetate ester. A two-pronged strategy...

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Τόπος έκδοσης:ACS Med Chem Lett
Κύριοι συγγραφείς: Tumey, L. Nathan, Leverett, Carolyn A., Vetelino, Beth, Li, Fengping, Rago, Brian, Han, Xiaogang, Loganzo, Frank, Musto, Sylvia, Bai, Guoyun, Sukuru, Sai Chetan K., Graziani, Edmund I., Puthenveetil, Sujiet, Casavant, Jeffrey, Ratnayake, Anokha, Marquette, Kimberly, Hudson, Sarah, Doppalapudi, Venkata Ramana, Stock, Joseph, Tchistiakova, Lioudmila, Bessire, Andrew J., Clark, Tracey, Lucas, Judy, Hosselet, Christine, O’Donnell, Christopher J., Subramanyam, Chakrapani
Μορφή: Artigo
Γλώσσα:Inglês
Έκδοση: American Chemical Society 2016
Διαθέσιμο Online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5108037/
https://ncbi.nlm.nih.gov/pubmed/27882194
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00195
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