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. 2001 Mar 13;98(6):2967–2972. doi: 10.1073/pnas.061028898

Table 1.

Kinetic inhibition of the three primary protease activities of the 20S proteasome by Z-specific inhibitors

Inhibitor kobs/[I] (1/M)
Suc-LLVY-MCA Boc-LRR-MCA Z-LLE-MCA
Ac-PRLN-VS ND 1,572  ± 3 (0.2–2 μM) ND
Ac-YRLN-VS ND 1,530  ± 1 (0.2–5 μM) ND
Ac-PKLN-VS ND 584  ± 3 (0.5–10 μM) ND
Ac-YKLN-VS ND 456  ± 2 (0.5–10 μM) ND
Ac-PRKN-VS ND 2,149  ± 4 (0.5–5 μM) ND
Ac-YRKN-VS 5.4 ± 0.4 (100–500 μM) 1,442  ± 7 (1–5 μM) 13.9 ± 0.5 (100–500 μM)

ND indicates no inhibition of substrate hydrolysis was observed at concentrations as high as 100 μM.