Structural basis for potency differences between GDF8 and GDF11

BMC Biol. 2017 Mar 3;15(1):19. doi: 10.1186/s12915-017-0350-1.

Abstract

Background: Growth/differentiation factor 8 (GDF8) and GDF11 are two highly similar members of the transforming growth factor β (TGFβ) family. While GDF8 has been recognized as a negative regulator of muscle growth and differentiation, there are conflicting studies on the function of GDF11 and whether GDF11 has beneficial effects on age-related dysfunction. To address whether GDF8 and GDF11 are functionally identical, we compared their signaling and structural properties.

Results: Here we show that, despite their high similarity, GDF11 is a more potent activator of SMAD2/3 and signals more effectively through the type I activin-like receptor kinase receptors ALK4/5/7 than GDF8. Resolution of the GDF11:FS288 complex, apo-GDF8, and apo-GDF11 crystal structures reveals unique properties of both ligands, specifically in the type I receptor binding site. Lastly, substitution of GDF11 residues into GDF8 confers enhanced activity to GDF8.

Conclusions: These studies identify distinctive structural features of GDF11 that enhance its potency, relative to GDF8; however, the biological consequences of these differences remain to be determined.

Keywords: Ligands; Myostatin; Receptor; Structure; Transforming growth factor β (TGFβ).

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Bone Morphogenetic Proteins / antagonists & inhibitors
  • Bone Morphogenetic Proteins / chemistry*
  • Bone Morphogenetic Proteins / metabolism
  • Cells, Cultured
  • Crystallography, X-Ray
  • Follistatin / metabolism
  • Genes, Reporter
  • Growth Differentiation Factors / antagonists & inhibitors
  • Growth Differentiation Factors / chemistry*
  • Growth Differentiation Factors / metabolism
  • Humans
  • Injections, Intravenous
  • Ligands
  • Luciferases / metabolism
  • Mice
  • Models, Molecular
  • Myoblasts / metabolism
  • Myocardium / metabolism
  • Myostatin / antagonists & inhibitors
  • Myostatin / chemistry*
  • Myostatin / metabolism*
  • Phosphorylation
  • Protein Binding
  • Protein Serine-Threonine Kinases / metabolism
  • Receptor, Transforming Growth Factor-beta Type I
  • Receptors, Transforming Growth Factor beta / metabolism
  • Sequence Alignment
  • Signal Transduction
  • Smad Proteins / metabolism
  • Structural Homology, Protein
  • Structure-Activity Relationship

Substances

  • Bone Morphogenetic Proteins
  • Follistatin
  • GDF11 protein, human
  • Growth Differentiation Factors
  • Ligands
  • Myostatin
  • Receptors, Transforming Growth Factor beta
  • Smad Proteins
  • Luciferases
  • Protein Serine-Threonine Kinases
  • Receptor, Transforming Growth Factor-beta Type I