Follistatin-based ligand trap ACE-083 induces localized hypertrophy of skeletal muscle with functional improvement in models of neuromuscular disease

Sci Rep. 2019 Aug 6;9(1):11392. doi: 10.1038/s41598-019-47818-w.

Abstract

Skeletal muscle is under inhibitory homeostatic regulation by multiple ligands of the transforming growth factor-β (TGFβ) superfamily. Follistatin is a secreted protein that promotes muscle growth and function by sequestering these ligands extracellularly. In the present study, we evaluated the potential of ACE-083 - a locally acting, follistatin-based fusion protein - as a novel therapeutic agent for focal or asymmetric myopathies. Characterization of ACE-083 in vitro revealed its high affinity for heparin and extracellular matrix while surface plasmon resonance and cell-based assays confirmed that ACE-083 binds and potently neutralizes myostatin, activin A, activin B and growth differentiation factor 11 (GDF11). Intramuscular administration of ACE-083 caused localized, dose-dependent hypertrophy of the injected muscle in wild-type mice and mouse models of Charcot-Marie-Tooth disease (CMT) and Duchenne muscular dystrophy, with no evidence of systemic muscle effects or endocrine perturbation. Importantly, ACE-083 also increased the force of isometric contraction in situ by the injected tibialis anterior muscle in wild-type mice and disease models and increased ankle dorsiflexion torque in CMT mice. Our results demonstrate the potential of ACE-083 as a therapeutic agent for patients with CMT, muscular dystrophy and other disorders with focal or asymmetric muscle atrophy or weakness.

MeSH terms

  • Activins / metabolism
  • Animals
  • Bone Morphogenetic Proteins / metabolism
  • Charcot-Marie-Tooth Disease / drug therapy*
  • Charcot-Marie-Tooth Disease / pathology
  • Disease Models, Animal
  • Follistatin / genetics
  • Follistatin / pharmacology*
  • Follistatin / therapeutic use
  • Growth Differentiation Factors / metabolism
  • Humans
  • Hypertrophy / chemically induced
  • Ligands
  • Male
  • Mice
  • Mice, Inbred mdx
  • Muscle Strength / drug effects
  • Muscle, Skeletal / drug effects*
  • Muscle, Skeletal / pathology
  • Muscular Dystrophy, Duchenne / drug therapy*
  • Muscular Dystrophy, Duchenne / pathology
  • Myostatin / metabolism
  • Receptors, IgG / genetics
  • Receptors, IgG / therapeutic use
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / pharmacology*
  • Recombinant Fusion Proteins / therapeutic use

Substances

  • Bone Morphogenetic Proteins
  • FST protein, human
  • Follistatin
  • Gdf11 protein, mouse
  • Growth Differentiation Factors
  • Ligands
  • Mstn protein, mouse
  • Myostatin
  • Receptors, IgG
  • Recombinant Fusion Proteins
  • activin A
  • activin B
  • Activins