Platelet GPVI: a target for antithrombotic therapy?!

Trends Pharmacol Sci. 2012 Nov;33(11):583-90. doi: 10.1016/ Epub 2012 Aug 15.


Platelet activation is a key step in the pathogenesis of ischemic cardio- and cerebrovascular diseases, which represent the leading causes of death and severe disability worldwide. Although existing antiplatelet drugs have proved beneficial in the clinic, their use is limited by their inherent effect on primary hemostasis, making the identification of novel pharmacological targets for platelet inhibition an important goal of cardiovascular research. In recent years, the central activating platelet collagen receptor, glycoprotein (GP) VI, has emerged as a promising antithrombotic target because its blockade or antibody-mediated depletion in circulating platelets was shown to effectively inhibit experimental thrombosis and thromboinflammatory disease states, such as stroke, without affecting hemostatic plug formation. In this review, we summarize the most important recent developments in understanding of GPVI function in hemostasis and thrombotic/inflammatory diseases and discuss the potential use of anti-GPVI agents to treat these pathologies in humans.

Publication types

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

MeSH terms

  • Animals
  • Blood Platelets / metabolism
  • Humans
  • Platelet Activation
  • Platelet Membrane Glycoproteins / antagonists & inhibitors
  • Platelet Membrane Glycoproteins / chemistry
  • Platelet Membrane Glycoproteins / genetics
  • Platelet Membrane Glycoproteins / metabolism*
  • Protein Structure, Tertiary
  • Thrombosis / drug therapy*
  • Thrombosis / metabolism


  • Platelet Membrane Glycoproteins
  • platelet membrane glycoprotein VI