Secondary substrate-binding exosite in the serine protease domain of activated protein C important for cleavage at Arg-506 but not at Arg-306 in factor Va

J Biol Chem. 2001 Jun 22;276(25):23105-8. doi: 10.1074/jbc.M103138200. Epub 2001 Apr 17.

Abstract

Proteolytic inactivation of activated factor V (FVa) by activated protein C (APC) is a key reaction in the regulation of hemostasis. We now demonstrate the importance of a positive cluster in loop 37 of the serine protease (SP) domain of APC for the degradation of FVa. Lysine residues in APC at positions 37, 38, and 39 form a secondary binding site for FVa, which is important for cleavage of FVa at Arg-506 while having no effect on Arg-306 cleavage. In contrast, topological neighbors Lys-62, Lys-63, and Arg-74 in APC appear of minor importance in FVa degradation. This demonstrates that secondary binding exosites of APC specifically guide the proteolytic action of APC, resulting in a more favorable degradation of the 506-507 peptide bond as compared with the 306-307 bond.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arginine / metabolism*
  • Binding Sites
  • Catalysis
  • Factor Va / metabolism*
  • Humans
  • Hydrolysis
  • Kinetics
  • Protein C / chemistry
  • Protein C / metabolism*
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Serine Endopeptidases / chemistry
  • Serine Endopeptidases / metabolism*
  • Structure-Activity Relationship

Substances

  • Protein C
  • Recombinant Proteins
  • Factor Va
  • Arginine
  • Serine Endopeptidases