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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5108037/
https://www.ncbi.nlm.nih.gov/pubmed/27882194
http://dx.doi.org/10.1021/acsmedchemlett.6b00195

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