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. Author manuscript; available in PMC: 2011 Sep 13.
Published in final edited form as: Nature. 2009 Sep 16;461(7264):621–626. doi: 10.1038/nature08357

Figure 2. Kinetic analysis of inactivation of Mtb 20SOG and human proteasomes (Hu20S) by oxathiazol-2-ones.

Figure 2

(a) Mtb20SOG (0.23 nM) was pre-treated with DMSO, GL5 (5 μM), salinosporamide A (NPI-0052, 10 nM), or bortezomib (2.7 μM) for 3 hours and assayed, then dialyzed against assay buffer overnight and assayed again. (b), (c) Plots of kobs as function of inhibitor concentration for GL5 (b) and HT1171 (c). Values for kobs, derived from the data in Fig S4, were plotted against inhibitor concentration [I]. (d) Kinetic parameters and partition ratios of GL5 and HT1171, determined as in Figs. S3 and S4. Kobs/[I] is second-order rate constant of inactivation. Partition ratios for human proteasomes refer to the β5 subunit. Standard errors were <10%.