嵌合微管破坏剂。
Chimeric microtubule disruptors.
机构信息
Medicinal Chemistry & Sterix Ltd., Department of Pharmacy & Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK.
出版信息
Chem Commun (Camb). 2010 May 7;46(17):2907-9. doi: 10.1039/c002558e. Epub 2010 Mar 20.
DOI:10.1039/c002558e
PMID:20386818
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.
摘要
一种嵌合方法被用于发现具有优异体外活性和口服生物利用度的微管破坏剂；通过蛋白质 X 射线晶体学研究，发现了与碳酸酐酶的配体-蛋白相互作用，从而提高了生物利用度。在肿瘤异种移植模型中对代表性嵌合体进行给药，证实了该类药物的优异治疗潜力。
Zotero 插件