Chimeric microtubule disruptors
Copyright policy )Chimeric microtubule disruptors
A chimeric approach is used to discover microtubule disruptors with excellent in vitro activity and oral bioavailability; a ligand-protein interaction with carbonic anhydrase that enhances bioavailability is characterised by protein X-ray crystallography. Dosing of a representative chimera in a tumour xenograft model confirms the excellent therapeutic potential of the class.
- St Mary's Hospital United Kingdom
- Imperial College London United Kingdom
- University of Bath United Kingdom
Binding Sites, Mice, Nude, Antineoplastic Agents, Crystallography, X-Ray, Ligands, Carbonic Anhydrase II, Xenograft Model Antitumor Assays, Tubulin Modulators, Mice, Cell Line, Tumor, Animals, Humans, Computer Simulation, Carbonic Anhydrase Inhibitors
Binding Sites, Mice, Nude, Antineoplastic Agents, Crystallography, X-Ray, Ligands, Carbonic Anhydrase II, Xenograft Model Antitumor Assays, Tubulin Modulators, Mice, Cell Line, Tumor, Animals, Humans, Computer Simulation, Carbonic Anhydrase Inhibitors
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