Triggered Drug Release from an Antibody–Drug Conjugate Using Fast 'Click-to-Release' Chemistry in Mice
| Autor: | Sander M. J. van Duijnhoven, Marc S. Robillard, Laurens H. J. Kleijn, Freek J. M. Hoeben, Raffaella Rossin, Ron M. Versteegen, Wolter ten Hoeve, Henk M. Janssen |
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| Přispěvatelé: | Macromolecular and Organic Chemistry |
| Rok vydání: | 2016 |
| Předmět: |
Antibody-drug conjugate
Immunoconjugates Drug Liberation Biomedical Engineering Pharmaceutical Science Bioengineering Pharmacology SDG 3 – Goede gezondheid en welzijn 010402 general chemistry 01 natural sciences Mice Elimination reaction SDG 3 - Good Health and Well-being Cell Line Tumor medicine Animals Humans Doxorubicin Mice Inbred BALB C 010405 organic chemistry Chemistry Organic Chemistry In vitro 0104 chemical sciences Pyridazines body regions Kinetics Click chemistry Biophysics Click Chemistry Female Bioorthogonal chemistry Biotechnology medicine.drug Conjugate |
| Zdroj: | Bioconjugate Chemistry, 27(7), 1697-1706. American Chemical Society |
| ISSN: | 1520-4812 1043-1802 |
| Popis: | The use of a bioorthogonal reaction for the selective cleavage of tumor-bound antibody-drug conjugates (ADCs) would represent a powerful new tool for ADC therapy, as it would not rely on the currently used intracellular biological activation mechanisms, thereby expanding the scope to noninternalizing cancer targets. Here we report that the recently developed inverse-electron-demand Diels-Alder pyridazine elimination reaction can provoke rapid and self-immolative release of doxorubicin from an ADC in vitro and in tumor-bearing mice. |
| Databáze: | OpenAIRE |
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