1 Matching Annotations
  1. May 2024
    1. clearly higher and faster fluorescence increase was observed in the sample treated with CTSB than in the samples treated with other proteases, which matches the reported CTSB-activated drug release profiles of ADCs bearing val-cit linkers.21

      Well... This is the opposite of what ref 21 says!!! Again, see this quote from ref 21:

      Despite the widespread use of protease-specific peptide cleavage (11), little is known about the determinants of the efficacy of VC-based ADCs. Here, we report an analysis of VC linker-based ADCs. We found that removal of cathepsin B did not affect the activity of ADCs and that proteases other than cathepsin B can also cleave the VC linker with varying degrees of efficiency. In addition, we show that alternative mechanisms could account for ADC efficacy independent of linker cleavage by proteases.

      and in fact Fig S7 shows increases for all proteases; the main difference is in the saturation value reached and not in the kinetics, which does not suggest specificity.