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Title | The binding mode of epothilone A on alpha,beta-tubulin by electron crystallography. |
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Journal, issue, pages | Science, Vol. 305, Issue 5685, Page 866-869, Year 2004 |
Publish date | Aug 6, 2004 |
Authors | James H Nettles / Huilin Li / Ben Cornett / Joseph M Krahn / James P Snyder / Kenneth H Downing / |
PubMed Abstract | The structure of epothilone A, bound to alpha,beta-tubulin in zinc-stabilized sheets, was determined by a combination of electron crystallography at 2.89 angstrom resolution and nuclear magnetic ...The structure of epothilone A, bound to alpha,beta-tubulin in zinc-stabilized sheets, was determined by a combination of electron crystallography at 2.89 angstrom resolution and nuclear magnetic resonance-based conformational analysis. The complex explains both the broad-based epothilone structure-activity relationship and the known mutational resistance profile. Comparison with Taxol shows that the longstanding expectation of a common pharmacophore is not met, because each ligand exploits the tubulin-binding pocket in a unique and independent manner. |
External links | Science / PubMed:15297674 |
Methods | EM (electron crystallography) |
Resolution | 2.89 Å |
Structure data | PDB-1tvk: |
Chemicals | ChemComp-GTP: ChemComp-GDP: ChemComp-EP: |
Source |
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Keywords | CELL CYCLE / STRUCTURAL PROTEIN / epothilone; taxol; ligand interactions |