Daunorubicin reduces MBNL1 sequestration caused by CUG-repeat expansion and rescues cardiac dysfunctions in a Drosophila model of myotonic dystrophy

Dis Model Mech. 2018 Apr 23;11(4):dmm032557. doi: 10.1242/dmm.032557.

Abstract

Myotonic dystrophy (DM) is a dominantly inherited neuromuscular disorder caused by expression of mutant myotonin-protein kinase (DMPK) transcripts containing expanded CUG repeats. Pathogenic DMPK RNA sequesters the muscleblind-like (MBNL) proteins, causing alterations in metabolism of various RNAs. Cardiac dysfunction represents the second most common cause of death in DM type 1 (DM1) patients. However, the contribution of MBNL sequestration in DM1 cardiac dysfunction is unclear. We overexpressed Muscleblind (Mbl), the DrosophilaMBNL orthologue, in cardiomyocytes of DM1 model flies and observed a rescue of heart dysfunctions, which are characteristic of these model flies and resemble cardiac defects observed in patients. We also identified a drug - daunorubicin hydrochloride - that directly binds to CUG repeats and alleviates Mbl sequestration in Drosophila DM1 cardiomyocytes, resulting in mis-splicing rescue and cardiac function recovery. These results demonstrate the relevance of Mbl sequestration caused by expanded-CUG-repeat RNA in cardiac dysfunctions in DM1, and highlight the potential of strategies aimed at inhibiting this protein-RNA interaction to recover normal cardiac function.

Keywords: Daunorubicin; Drosophila; Muscleblind; Myotonic dystrophy; Trinucleotide repeat disorder.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alternative Splicing / genetics
  • Animals
  • Daunorubicin / pharmacology*
  • Disease Models, Animal
  • Drosophila Proteins / genetics
  • Drosophila Proteins / metabolism*
  • Drosophila melanogaster / drug effects
  • Drosophila melanogaster / metabolism*
  • Heart / drug effects
  • Heart / physiopathology*
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism
  • Myotonic Dystrophy / genetics*
  • Myotonic Dystrophy / physiopathology*
  • Nuclear Proteins / genetics
  • Nuclear Proteins / metabolism*
  • Protein Binding / drug effects
  • RNA Stability / drug effects
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Reproducibility of Results
  • Survival Analysis
  • Trinucleotide Repeat Expansion / genetics*

Substances

  • Drosophila Proteins
  • Nuclear Proteins
  • RNA, Messenger
  • mbl protein, Drosophila
  • Daunorubicin