P-selectin antagonism in inflammatory disease

Curr Pharm Des. 2010;16(37):4113-8. doi: 10.2174/138161210794519192.


Inflammation plays a fundamental role in many chronic diseases, including atherosclerosis associated cardiovascular disease. Adhesion of immune cells plays a critical role in the inflammatory response and indeed the pathophysiology of inflammatory related diseases. P-selectin is an inflammatory adhesion molecule, enabling the recruitment of leukocytes to the endothelium and to activated platelets involved with the growing thrombus. P-selectin is critical in the progression of atherosclerosis as evidenced by knockout animal models where P-selectin knockout mice crossed with apoE deficient mice exhibit significantly reduced atherosclerosis and leukocyte recruitment in the plaque. A soluble form of P-selectin also exists, which may have pro-atherogenic and pro-thrombotic effects. Thus targeting of P-selectin remains a strong clinical candidate for developing novel therapeutic strategies in inflammatory diseases. This review will discuss the role of P-selectin and describe the function of P-selectin antagonists as clinical targets.

Publication types

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

MeSH terms

  • Animals
  • Atherosclerosis / drug therapy
  • Atherosclerosis / immunology
  • Atherosclerosis / physiopathology
  • Disease Progression
  • Humans
  • Inflammation / drug therapy
  • Inflammation / immunology*
  • Inflammation / physiopathology
  • Leukocytes / immunology
  • Leukocytes / physiology
  • Membrane Glycoproteins / immunology
  • Membrane Glycoproteins / metabolism
  • Mice
  • Mice, Knockout
  • Molecular Targeted Therapy
  • P-Selectin / antagonists & inhibitors*
  • P-Selectin / immunology
  • P-Selectin / physiology*
  • Platelet Activation
  • Thrombosis / immunology
  • Thrombosis / physiopathology


  • Membrane Glycoproteins
  • P-Selectin
  • P-selectin ligand protein