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

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

23 Citations (Scopus)

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)	2907-9
Number of pages	3
Journal	Chemical Communications
Volume	46
Issue number	17
DOIs	https://doi.org/10.1039/c002558e
Publication status	Published - 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.",

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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

Y1 - 2010

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.

U2 - 10.1039/c002558e

DO - 10.1039/c002558e

M3 - Article

C2 - 20386818

SN - 1364-548X

VL - 46

SP - 2907

EP - 2909

JO - Chemical Communications

JF - Chemical Communications

IS - 17

ER -

Chimeric microtubule disruptors

Abstract

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