Resistance by allostery: a novel perspective for eg5-targeted drug design

J Med Chem. 2013 Aug 22;56(16):6314-6. doi: 10.1021/jm401071u. Epub 2013 Jul 30.

Abstract

Talapatra et al. elucidated the molecular basis of resistance by characterizing the binding interactions between Eg5 and the allosteric inhibitor SB743921. The investigation, employing biochemical, biophysical, and structural analyses, made path-breaking revelations in Eg5 studies and discussed a novel phenomenon "resistance by allostery", which could have far-reaching consequences from a rational drug design perspective.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allosteric Regulation
  • Benzamides / chemistry
  • Benzamides / pharmacology
  • Chromones / chemistry
  • Chromones / pharmacology
  • Drug Design*
  • Humans
  • Kinesins / chemistry
  • Kinesins / drug effects*
  • Models, Molecular

Substances

  • Benzamides
  • Chromones
  • KIF11 protein, human
  • SB 743921
  • Kinesins