Chimeric microtubule disruptors

Mathew P. Leese; Fabrice Jourdan; Meriel R. Kimberley; Gyles E. Cozier; Nethaji Thiyagarajan; Chloe Stengel; Sandra Regis-Lydi; Paul A. Foster; Simon P. Newman; K. Ravi Acharya; Eric Ferrandis; Atul Purohit; Michael J. Reed; Barry V. L. Potter

doi:10.1039/c002558e

Chimeric microtubule disruptors

Mathew P. Leese, Fabrice Jourdan, Meriel R. Kimberley, Gyles E. Cozier, Nethaji Thiyagarajan, Chloe Stengel, Sandra Regis-Lydi, Paul A. Foster, Simon P. Newman, K. Ravi Acharya, Eric Ferrandis, Atul Purohit, Michael J. Reed, Barry V. L. Potter

Department of Life Sciences

Research output: Contribution to journal › Article › peer-review

24 Citations (SciVal)

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.

Original language	English
Pages (from-to)	2907-2909
Journal	Chemical Communications
Volume	46
Issue number	17
DOIs	https://doi.org/10.1039/c002558e
Publication status	Published - 7 May 2010

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title = "Chimeric microtubule disruptors",

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.",

author = "Leese, \{Mathew P.\} and Fabrice Jourdan and Kimberley, \{Meriel R.\} and Cozier, \{Gyles E.\} and Nethaji Thiyagarajan and Chloe Stengel and Sandra Regis-Lydi and Foster, \{Paul A.\} and Newman, \{Simon P.\} and Acharya, \{K. Ravi\} and Eric Ferrandis and Atul Purohit and Reed, \{Michael J.\} and Potter, \{Barry V. L.\}",

year = "2010",

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doi = "10.1039/c002558e",

language = "English",

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T1 - Chimeric microtubule disruptors

AU - Leese, Mathew P.

AU - Jourdan, Fabrice

AU - Kimberley, Meriel R.

AU - Cozier, Gyles E.

AU - Thiyagarajan, Nethaji

AU - Stengel, Chloe

AU - Regis-Lydi, Sandra

AU - Foster, Paul A.

AU - Newman, Simon P.

AU - Acharya, K. Ravi

AU - Ferrandis, Eric

AU - Purohit, Atul

AU - Reed, Michael J.

AU - Potter, Barry V. L.

PY - 2010/5/7

Y1 - 2010/5/7

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/77950939804

UR - http://dx.doi.org/10.1039/c002558e

U2 - 10.1039/c002558e

DO - 10.1039/c002558e

M3 - Article

SN - 1359-7345

VL - 46

SP - 2907

EP - 2909

JO - Chemical Communications

JF - Chemical Communications

IS - 17

ER -

Chimeric microtubule disruptors

Abstract

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