Research

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
CreatorsLeese, 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.
DOI10.1039/c002558e
DepartmentsFaculty of Science > Pharmacy & Pharmacology
Faculty of Science > Biology & Biochemistry
RefereedYes
StatusPublished
ID Code18739

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