This is a cathepsin cleavable linker used in the construction of antibody drug conjugates (ADC & Bioconjugation).
特點和優勢
Val-Cit-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADC). The Val-Cit is specifically cleaved by cathepsin B. The Boc group can be deprotected under acidic conditions to generate a free amine group. As this enzyme is only present in the lysosome the ADC payload will be release only in the cell.
European journal of medicinal chemistry, 199, 112364-112364 (2020-05-14)
Cryptophycin-52 (CR52), a tubulin inhibitor, exhibits promising antitumor activity in vitro (picomolar level) and in mouse xenograft models. However, the narrow therapeutic window in clinical trials limits its further development. Antibody-drug conjugate (ADC), formed by coupling cytotoxic compound (payload) to an
International journal of nanomedicine, 16, 2443-2459 (2021-04-06)
Specific modifications to carriers to achieve targeted delivery of chemotherapeutics into malignant tissues are a critical point for efficient diagnosis and therapy. In this case, bovine serum albumin (BSA) was conjugated with cetuximab-valine-citrulline (vc)-doxorubicin (DOX) to target epidermal growth factor
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