Anticoagulant and antithrombotic properties of platelet protease nexin-1

Blood. 2010 Jan 7;115(1):97-106. doi: 10.1182/blood-2009-04-217240. Epub 2009 Oct 23.

Abstract

Protease nexin-1 (PN-1) is a serpin that inhibits plasminogen activators, plasmin, and thrombin. PN-1 is barely detectable in plasma but is expressed by platelets. Here, we studied platelet PN-1 in resting and activated conditions and its function in thrombosis. Studies on human platelets from healthy donors and from patients with a Gray platelet syndrome demonstrate that PN-1 is present both at the platelet surface and in alpha-granules. The role of PN-1 was investigated in vitro using human platelets incubated with a blocking antibody and using platelets from PN-1-deficient mice. Both approaches indicate that platelet PN-1 is active on thrombin and urokinase-type plasminogen activator. Blockade and deficiency of platelet PN-1 result in accelerated and increased tissue factor-induced thrombin generation as indicated by calibrated automated thrombography. Moreover, platelets from PN-1-deficient mice respond to subthreshold doses of thrombin, as assessed by P-selectin expression and platelet aggregation. Thrombus formation, induced ex vivo by collagen in blood flow conditions and in vivo by FeCl(3)-induced injury, is significantly increased in PN-1-deficient mice, demonstrating the antithrombotic properties of platelet PN-1. Platelet PN-1 is thus a key player in the thrombotic process, whose negative regulatory role has been, up to now, markedly underestimated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Amyloid beta-Protein Precursor / metabolism*
  • Animals
  • Anticoagulants / metabolism*
  • Antithrombins / metabolism*
  • Blood Circulation / drug effects
  • Blood Platelets / drug effects
  • Blood Platelets / enzymology*
  • Blood Platelets / metabolism
  • Blood Vessels / drug effects
  • Blood Vessels / enzymology
  • Blood Vessels / pathology
  • Blood Vessels / physiopathology
  • Cell Membrane / drug effects
  • Cell Membrane / enzymology
  • Collagen / pharmacology
  • Glycosaminoglycans / metabolism
  • Humans
  • Mice
  • Platelet Aggregation / drug effects
  • Platelet-Rich Plasma / metabolism
  • Protease Nexins
  • Receptors, Cell Surface / metabolism*
  • Serpin E2
  • Thrombin / antagonists & inhibitors
  • Thromboplastin / metabolism
  • Thrombosis / enzymology
  • Thrombosis / pathology
  • Thrombosis / physiopathology
  • Time Factors
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors

Substances

  • Amyloid beta-Protein Precursor
  • Anticoagulants
  • Antithrombins
  • Glycosaminoglycans
  • Protease Nexins
  • Receptors, Cell Surface
  • SERPINE2 protein, human
  • Serpin E2
  • Collagen
  • Thromboplastin
  • Thrombin
  • Urokinase-Type Plasminogen Activator