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. Author manuscript; available in PMC: 2011 Aug 27.
Published in final edited form as: Chem Biol. 2010 Aug 27;17(8):795–801. doi: 10.1016/j.chembiol.2010.05.027

Figure 4. Analysis of β5t Substrate Specificity in Juvenile Murine Thymus Lysates by Competitive Activity-Based Profiling with ABP 4.

Figure 4

(A) Lysates were exposed to increasing concentrations Lactacystin or MG132; residual β5t activity was stained with ABP 4 and visualized by in-gel fluorescence detection. The inhibitors are not reactive toward the β5t activity.

(B) Bortezomib efficiently inhibits β5, β5i, β1, and β1i activity but not β5t. NC005 specifically targets β5 (indicated by the gray arrow) but not β5t. The mixed inhibitor containing the boronic ester warhead equipped with the epoxomicin tail efficiently blocks β5t.

(C) In analogy to (B), installation of the epoxomicin IleIleThrLeu peptide targeting motif to the vinyl sulphone warhead affords a potent inhibitor of the β5t activity.

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