Chimeric microtubule disruptors
Reference:
Leese, M. P., Jourdan, F., Kimberley, M. R., Cozier, G. E., Thiyagarajan, N., Stengel, C., Regis-Lydi, S., Foster, P. A., Newman, S. P., Acharya, K. R., Ferrandis, E., Purohit, A., Reed, M. J. and Potter, B. V. L., 2010. Chimeric microtubule disruptors. Chemical Communications, 46 (17), pp. 2907-2909.
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Official URL:
http://dx.doi.org/10.1039/c002558e
Abstract
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.
Details
| Item Type | Articles |
| Creators | Leese, M. P., Jourdan, F., Kimberley, M. R., Cozier, G. E., Thiyagarajan, N., Stengel, C., Regis-Lydi, S., Foster, P. A., Newman, S. P., Acharya, K. R., Ferrandis, E., Purohit, A., Reed, M. J. and Potter, B. V. L. |
| DOI | 10.1039/c002558e |
| Departments | Faculty of Science > Pharmacy & Pharmacology Faculty of Science > Biology & Biochemistry |
| Refereed | Yes |
| Status | Published |
| ID Code | 18739 |
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