Relationship between propeptide pH unfolding and inhibitory ability during ProDer p 1 activation mechanism

J Mol Biol. 2007 Nov 16;374(1):170-85. doi: 10.1016/j.jmb.2007.08.025. Epub 2007 Aug 21.

Abstract

The major allergen Der p 1 of the house dust mite Dermatophagoides pteronyssinus is a papain-like cysteine protease (CA1) produced as an inactive precursor and associated with allergic diseases. The propeptide of Der p 1 exhibits a specific fold that makes it unique in the CA1 propeptide family. In this study, we investigated the activation steps involved in the maturation of the recombinant protease Der p 1 expressed in Pichia pastoris and the interaction of the full-length and truncated soluble propeptides with their parent enzyme in terms of activity inhibition and BIAcore interaction analysis. According to our results, the activation of protease Der p 1 is a multistep mechanism that is characterized by at least two intermediates. The propeptide strongly inhibits unglycosylated and glycosylated recombinant Der p 1 (K(D)=7 nM) at neutral pH. This inhibition is pH dependent. It decreases from pH 7 to pH 4 and can be related to conformational changes of the propeptide characterized by an increase of its flexibility and formation of a molten globule state. Our results indicate that activation of the zymogen at pH 4 is a compromise between activity preservation and propeptide unfolding.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antigens, Dermatophagoides / genetics
  • Antigens, Dermatophagoides / immunology
  • Antigens, Dermatophagoides / metabolism*
  • Arthropod Proteins
  • Circular Dichroism
  • Computer Simulation
  • Cysteine Endopeptidases
  • Dermatophagoides pteronyssinus / enzymology
  • Dermatophagoides pteronyssinus / immunology
  • Enzyme Precursors
  • Fluorescence
  • Glycosylation
  • Hydrogen-Ion Concentration
  • Peptide Fragments / chemistry*
  • Peptide Fragments / pharmacology*
  • Pichia / genetics
  • Pichia / metabolism
  • Protein Folding*
  • Protein Processing, Post-Translational
  • Recombinant Proteins
  • Surface Plasmon Resonance

Substances

  • Antigens, Dermatophagoides
  • Arthropod Proteins
  • Enzyme Precursors
  • Peptide Fragments
  • Recombinant Proteins
  • Cysteine Endopeptidases
  • Dermatophagoides pteronyssinus antigen p 1