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. 2008 Dec;3(12):1844-7.
doi: 10.1002/cmdc.200800288.

Differences in paclitaxel and docetaxel interactions with tubulin detected by mutagenesis of yeast tubulin

Robert D Winefield  1 , Ruth A Entwistle, Travis B Foland, Gerald H Lushington, Richard H Himes
Affiliations

Differences in paclitaxel and docetaxel interactions with tubulin detected by mutagenesis of yeast tubulin

Robert D Winefield et al. ChemMedChem. 2008 Dec.
No abstract available

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Figures

Figure 1
Figure 1
Effect of the H227N mutation on the assembly of yeast tubulin. The conditions of the experiment are described in the Experimental Section. A, strain BBBBB. B, strain BBBYB. Error bars refer to standard error of the mean.
Figure 2
Figure 2
Effect of the H227N mutation on the displacement of 3H-paclitaxel by docetaxel. The conditions of the experiment are described in the Experimental Section.
Figure 3
Figure 3
A molecular model showing the H227 and N227 residues in the tubulin-paclitaxel and tubulin-docetaxel complexes. The position of paclitaxel and residues interacting with it are shown (black) superimposed over docetaxel and residues interacting with it (green). Helices (purple), β-strands (yellow), and loops (light blue), are shown along with oxygen (red), nitrogen (dark blue), and hydrogen atoms (light blue spheres). Helices and β-strands are labeled sequentially according to the β-tubulin sequence along with the C-3' benzamido (a), the C-3' phenyl (b), and the C2-benzoyl phenyl groups (c) belonging to paclitaxel and docetaxel. In the BBBYB complexes formation of an H-bond between the N227 side chain and the carbonyl oxygen of the paclitaxel benzamido and the docetaxel carbamate groups is shown.
Scheme
Scheme
Structures of paclitaxel and docetaxel.
See this image and copyright information in PMC

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