The elusive role of the potential factor X cation-binding exosite-1 in substrate and inhibitor interactions

J Biol Chem. 2004 Jan 30;279(5):3671-9. doi: 10.1074/jbc.M309691200. Epub 2003 Oct 28.

Abstract

A number of studies suggest that blood-clotting factor X (FX) uses secondary site(s) to interact (as a substrate) with its activators. Numerous pieces of evidence also imply that, within prothrombinase (as an enzyme), activated FX (FXa) uses exosite(s) for cofactor Va and/or prothrombin recognition. Similarly, FXa exosite(s) seem to govern interaction with inhibitors. An obvious difference between FXa and thrombin resides within a region called exosite-1: positively charged in thrombin and clearly of opposite polarity in FXa. To investigate the role of this potential cation-binding exosite, we prepared a series of mutants within loops 34-40 and 70-80 of FX. Overall, the mutations induced relatively subtle, non-synergistic modulation. The potential exosite was dispensable for FX activation and is unlikely to constitute a critical region for factor Va binding, albeit it is clearly important for prothrombin activation. Our data also implicate loop 34-40 of FXa in the interaction with the tissue factor pathway inhibitor, in prevention of plasminogen activator inhibitor-1 binding, and in tempering inhibition by heparin-activated antithrombin. Compared with FX, mutants with reduced electrostatic potential potentiated thrombin production in FX-depleted plasma, whereas mutants with inverted electrostatic potential impeded clotting. Despite the definite consequences observed, disruption of the potential cation-binding exosite of FX had rather weak effects, far from what would be expected if this region was as crucial as in thrombin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antithrombins / chemistry
  • Cations
  • DNA, Complementary / metabolism
  • Enzyme Activation
  • Factor Va / chemistry
  • Factor X / chemistry*
  • Factor X / physiology
  • Factor Xa / chemistry
  • Heparin / chemistry
  • Humans
  • Hydrolysis
  • Kinetics
  • Models, Chemical
  • Models, Molecular
  • Molecular Sequence Data
  • Mutation
  • Protein Binding
  • Protein Structure, Tertiary
  • Prothrombin / chemistry
  • Static Electricity
  • Thrombin / chemistry*
  • Time Factors

Substances

  • Antithrombins
  • Cations
  • DNA, Complementary
  • Factor Va
  • Prothrombin
  • Factor X
  • Heparin
  • Thrombin
  • Factor Xa