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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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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2016
Acesso em linha: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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