Structural evidence for cooperative microtubule stabilization by Taxol and the endogenous dynamics regulator MAP4

ACS Chem Biol. 2012 Apr 20;7(4):744-52. doi: 10.1021/cb200403x. Epub 2012 Feb 6.

Abstract

Microtubules (MTs) composed of αβ-tubulin heterodimers are highly dynamic polymers, whose stability can be regulated by numerous endogenous and exogenous factors. Both the antimitotic drug Taxol and microtubule-associated proteins (MAPs) stabilize this dynamicity by binding to and altering the conformation of MTs. In the current study, amide hydrogen/deuterium exchange coupled with mass spectrometry (HDX-MS) was used to examine the structural and dynamic properties of the MT complex with the microtubule binding domain of MAP4 (MTB-MAP4) in the presence and absence of Taxol. The changes in the HDX levels indicate that MTB-MAP4 may bind to both the outside and the luminal surfaces of the MTs and that Taxol reduces both of these interactions. The MTB-MAP4 binding induces conformational rearrangements of α- and β-tubulin that promote an overall stabilization of MTs. Paradoxically, despite Taxol's negative effects on MAP4 interactions with the MTs, its binding to the MTB-MAP4-MT complex further reduces the overall deuterium incorporation, suggesting that a more stable complex is formed in the presence of the drug.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Humans
  • Microtubule-Associated Proteins / chemistry*
  • Microtubules / chemistry
  • Microtubules / drug effects*
  • Paclitaxel / chemistry
  • Paclitaxel / pharmacology*
  • Protein Binding
  • Protein Conformation
  • Protein Stability / drug effects

Substances

  • Microtubule-Associated Proteins
  • Paclitaxel