Hyperdynamic microtubules, cognitive deficits, and pathology are improved in tau transgenic mice with low doses of the microtubule-stabilizing agent BMS-241027

J Neurosci. 2012 May 23;32(21):7137-45. doi: 10.1523/JNEUROSCI.0188-12.2012.

Abstract

Tau is a microtubule (MT)-stabilizing protein that is altered in Alzheimer's disease (AD) and other tauopathies. It is hypothesized that the hyperphosphorylated, conformationally altered, and multimeric forms of tau lead to a disruption of MT stability; however, direct evidence is lacking in vivo. In this study, an in vivo stable isotope-mass spectrometric technique was used to measure the turnover, or dynamicity, of MTs in brains of living animals. We demonstrated an age-dependent increase in MT dynamics in two different tau transgenic mouse models, 3xTg and rTg4510. MT hyperdynamicity was dependent on tau expression, since a reduction of transgene expression with doxycycline reversed the MT changes. Treatment of rTg4510 mice with the epothilone, BMS-241027, also restored MT dynamics to baseline levels. In addition, MT stabilization with BMS-241027 had beneficial effects on Morris water maze deficits, tau pathology, and neurodegeneration. Interestingly, pathological and functional benefits of BMS-241027 were observed at doses that only partially reversed MT hyperdynamicity. Together, these data suggest that tau-mediated loss of MT stability may contribute to disease progression and that very low doses of BMS-241027 may be useful in the treatment of AD and other tauopathies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Brain / pathology
  • Cognition Disorders / complications
  • Cognition Disorders / drug therapy*
  • Cognition Disorders / metabolism
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Doxycycline / pharmacology
  • Drug Evaluation, Preclinical / methods
  • Drug Evaluation, Preclinical / psychology
  • Epothilones / pharmacology
  • Epothilones / therapeutic use*
  • Female
  • Hippocampus / drug effects
  • Hippocampus / pathology
  • Male
  • Maze Learning / drug effects
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Microtubules / drug effects
  • Microtubules / pathology*
  • Nerve Degeneration / drug therapy*
  • Tauopathies / complications
  • Tauopathies / drug therapy*
  • Tauopathies / genetics
  • Tauopathies / pathology
  • Tauopathies / psychology
  • Tubulin Modulators / pharmacology
  • Tubulin Modulators / therapeutic use*
  • tau Proteins / antagonists & inhibitors
  • tau Proteins / biosynthesis
  • tau Proteins / genetics
  • tau Proteins / physiology*

Substances

  • Epothilones
  • Tubulin Modulators
  • tau Proteins
  • Doxycycline
  • desoxyepothilone B