Increased biological activity of a recombinant factor IX variant carrying alanine at position +1

Protein Eng. 1990 Jul;3(7):629-33. doi: 10.1093/protein/3.7.629.

Abstract

In attempts to improve the post-translational modification and processing of recombinant factor IX (FIX) we have altered the cDNA sequence encoding pre-pro-FIX using site-directed mutagenesis and have expressed the variant cDNAs in BHK21 cells using a vaccinia-virus-derived vector. We find that substitution of the tyrosine residue at +1 for an alanine increases the biological activity of the recombinant molecules 2-fold. On the other hand, substitution of the proline at -3 for a valine results in no significant change to the specific activity of the protein. Other alterations to the N-terminus of the FIX proteins, in attempts to mimic other vitamin-K-dependent proteins, result in the failure to produce a secreted polypeptide. N-terminal sequence analysis of purified recombinant molecules reveals a correlation between specific activity and the efficiency of correct pro-sequence cleavage. gamma-Carboxylation analysis of purified recombinant proteins indicates that each molecule including unmutated FIX is completely gamma-carboxylated in this system. Thus the observed increase in biological activity of FIX variants containing an alanine at position +1 is not due to increased gamma-carboxylation but, at least in part, to more efficient pro-peptide cleavage.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alanine / genetics*
  • Amino Acid Sequence
  • Animals
  • Cells, Cultured
  • Chromosome Deletion
  • Cricetinae
  • DNA / analysis
  • Factor IX / genetics*
  • Factor IX / metabolism
  • Gene Expression
  • Genetic Variation*
  • Molecular Sequence Data
  • Recombinant Proteins*
  • Tyrosine / genetics*

Substances

  • Recombinant Proteins
  • Tyrosine
  • Factor IX
  • DNA
  • Alanine