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Cathepsin substrates as cleavable peptide linkers in bioconjugates, selected from a fluorescence quench combinatorial
1Department of Chemistry, University of California, One Shields Avenue, Davis, California 95616-5295, USA.
Bioconjugate Chemistry
|September 15, 1998
Abstract:
Several extended peptide substrates for the human liver enzymes cathepsin B and cathepsin D have been selected as cleavable linkers for lysosomal proteolysis of bioconjugates. A one-bead-one-peptide combinatorial library of 9(4) fluorogenic substrates was employed. We designed this library to explore a set of substrates containing nonionizable/nonoxidizable groups to meet the requirements of prelabeling [Li et al. (1994) Bioconjugate Chem. 5, 101-104] as well as to yield stable conjugates whose preparation is straightforward.