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. Author manuscript; available in PMC: 2011 Nov 1.
Published in final edited form as: Bioorg Med Chem. 2010 Aug 21;18(21):7611–7620. doi: 10.1016/j.bmc.2010.08.038

Figure 6. Structure and activity of compound 58H5-6.

Figure 6

A. Nuclear import of Alexa555-BSA-NLS cargo in the cell permeabilized nuclear import assay in the presence of 1% DMSO (negative control), 1% DMSO and 2 mM GMP-PNP (positive control) or 500 μM 58H5-6. Scale bar is 10 μm. B. Nuclear import of Alexa555-GST-M9 cargo in the cell permeabilized nuclear import assay in the presence of 1% DMSO (negative control), 1% DMSO and 1 mg/ml WGA (positive control) or 500 μM 58H5-6. Scale bar is 10 μm. C. Structure of 58H5-6. D. Dose-response curve of 58H5-6 in the cell permeabilized nuclear import assay using the importin α/β cargo Alexa555-BSA-NLS. E. The thermodynamically most stable conformation of 58H5-6 docked into an FxFG binding site on importin β. The 58H5-6 inhibitor (red) docked to importin β (green) is superimposed on the crystallographic structure of an FxFG peptide fragment (yellow).