Triggered Drug Release from an Antibody–Drug Conjugate Using Fast “Click-to-Release” Chemistry in Mice
…, RM Versteegen, MS Robillard
文献索引：Versteegen, Ron M.; Rossin, Raffaella; Ten Hoeve, Wolter; Janssen, Henk M.; Robillard, Marc S. Angewandte Chemie - International Edition, 2013 , vol. 52, # 52 p. 14112 - 14116 Angew. Chem., 2013 , vol. 125, # 52 p. 14362 - 14366,5
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 ...
