Fig. 5: Taccalonolide probes engage additional β-tubulin contacts. | Nature Communications

Fig. 5: Taccalonolide probes engage additional β-tubulin contacts.

From: Elucidating target specificity of the taccalonolide covalent microtubule stabilizers employing a combinatorial chemical approach

Fig. 5

a, b Effects of free taccalonolide AJ (2) and taccalonolide-fluorescein probes (6, 8, 11, 12) on the polymerization of purified porcine tubulin. a Concentration-dependent (5–20 μM) effects of 2 on tubulin polymerization with vehicle in black and 2 in shades of blue from lightest to darkest as concentration increases. The introduction of pivaloyl protecting groups in 8 (red) and 11 (green) diminish this activity even at equimolar concentrations with tubulin (20 μM). b The deprotected taccalonolide probes 6 (orange) or 12 (purple) are more potent than 2 (blue) or 11 (green) in their ability to polymerize purified tubulin. c–f Comparison of the published structure 5EZY (2 bound to β-tubulin) c with a model of β-tubulin docked to taccalonolide probes (6) d, (12) e, and (11) f. The selected H-bonds and salt bridges are displayed as yellow and magenta dashed lines, respectively. Source data are provided as a Source Data file.

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