Troponin activator augments muscle force in nemaline myopathy patients with nebulin mutations

J Med Genet. 2013 Jun;50(6):383-92. doi: 10.1136/jmedgenet-2012-101470. Epub 2013 Apr 9.

Abstract

Background: Nemaline myopathy-the most common non-dystrophic congenital myopathy-is caused by mutations in thin filament genes, of which the nebulin gene is the most frequently affected one. The nebulin gene codes for the giant sarcomeric protein nebulin, which plays a crucial role in skeletal muscle contractile performance. Muscle weakness is a hallmark feature of nemaline myopathy patients with nebulin mutations, and is caused by changes in contractile protein function, including a lower calcium-sensitivity of force generation. To date no therapy exists to treat muscle weakness in nemaline myopathy. Here, we studied the ability of the novel fast skeletal muscle troponin activator, CK-2066260, to augment force generation at submaximal calcium levels in muscle cells from nemaline myopathy patients with nebulin mutations.

Methods: Contractile protein function was determined in permeabilised muscle cells isolated from frozen patient biopsies. The effect of 5 μM CK-2066260 on force production was assessed.

Results: Nebulin protein concentrations were severely reduced in muscle cells from these patients compared to controls, while myofibrillar ultrastructure was largely preserved. Both maximal active tension and the calcium-sensitivity of force generation were lower in patients compared to controls. Importantly, CK-2066260 greatly increased the calcium-sensitivity of force generation-without affecting the cooperativity of activation-in patients to levels that exceed those observed in untreated control muscle.

Conclusions: Fast skeletal troponin activation is a therapeutic mechanism to augment contractile protein function in nemaline myopathy patients with nebulin mutations and with other neuromuscular diseases.

Keywords: Muscle disease.

Publication types

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

MeSH terms

  • Adult
  • Biopsy
  • Calcium / metabolism
  • Child, Preschool
  • Humans
  • Imidazoles / administration & dosage
  • Imidazoles / pharmacology*
  • Infant
  • Muscle Fibers, Skeletal / drug effects
  • Muscle Fibers, Skeletal / pathology
  • Muscle Proteins / genetics*
  • Muscle Strength / drug effects*
  • Mutation / genetics*
  • Myopathies, Nemaline / drug therapy
  • Myopathies, Nemaline / genetics
  • Myopathies, Nemaline / physiopathology*
  • Pyrazines / administration & dosage
  • Pyrazines / pharmacology*
  • Treatment Outcome
  • Troponin / drug effects
  • Troponin / metabolism*
  • Young Adult

Substances

  • Imidazoles
  • Muscle Proteins
  • Pyrazines
  • Troponin
  • nebulin
  • Calcium