Structures of soluble rabbit neprilysin complexed with phosphoramidon or thiorphan

Acta Crystallogr F Struct Biol Commun. 2019 Jun 1;75(Pt 6):405-411. doi: 10.1107/S2053230X19006046. Epub 2019 May 10.

Abstract

Neutral endopeptidase (neprilysin; NEP) is a proteinase that cleaves a wide variety of peptides and has been implicated in Alzheimer's disease, cardiovascular conditions, arthritis and other inflammatory diseases. The structure of the soluble extracellular domain (residues 55-750) of rabbit neprilysin was solved both in its native form at 2.1 Å resolution, and bound to the inhibitors phosphoramidon and thiorphan at 2.8 and 3.0 Å resolution, respectively. Consistent with the extracellular domain of human neprilysin, the structure reveals a large central cavity which contains the active site and the location for inhibitor binding.

Keywords: neprilysin; neutral endopeptidase; phosphoramidon; thiorphan.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Crystallography, X-Ray
  • Glycopeptides / chemistry
  • Glycopeptides / metabolism*
  • Models, Molecular*
  • Neprilysin / chemistry*
  • Neprilysin / metabolism*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / metabolism*
  • Protein Conformation
  • Rabbits
  • Substrate Specificity
  • Thiorphan / chemistry
  • Thiorphan / metabolism*

Substances

  • Glycopeptides
  • Protease Inhibitors
  • Thiorphan
  • Neprilysin
  • phosphoramidon