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Further optimization of the P4 (R) and P′ groups produces compounds showing high target potency and intrinsic selectivity over cathepsin B. Chemical syntheses and enzymatic activity assays are described by Newton et al. (2014) and the online supporting information, https://pubs.acs.org/doi/suppl/10.1021/jm501102h and https://pubs.acs.org/doi/suppl/10.1021/jm501102h/suppl_file/jm501102h_si_001.pdf.
