756487-16-8Relevant academic research and scientific papers
Monoclonal antibody mediated intracellular targeting of tallysomycin S 10b
Walker, Michael A.,King, H. Dalton,Dalterio, Richard A.,Trail, Pamela,Firestone, Raymond,Dubowchik, Gene M.
, p. 4323 - 4327 (2004)
The potency of tallysomycin S10b (TLM S10b) an analogue bleomycin was enhanced by up to 875-fold when it was conjugated to the internalizing antibody BR96. Attachment to the antibody is achieved via a Cathepsin B cleavable linker. The enhancement in potency is believed to be a result of cellular uptake of the conjugate upon antigen binding followed by rapid release of the drug inside the lysosome. This method provides a novel approach for increasing the potency and therapeutic index of nominally moderately-active cytotoxic agents.
