sPLA2-V inhibits EPCR anticoagulant and antiapoptotic properties by accommodating lysophosphatidylcholine or PAF in the hydrophobic groove

Blood. 2012 Mar 22;119(12):2914-21. doi: 10.1182/blood-2011-05-353409. Epub 2011 Dec 13.

Abstract

The endothelial protein C receptor (EPCR) plays an important role in cardiovascular disease by binding protein C/activated protein C (APC). EPCR structure contains a hydrophobic groove filled with an unknown phospholipid needed to perform its function. It has not been established whether lipid exchange takes place in EPCR as a regulatory mechanism of its activity. Our objective was to identify this phospholipid and to explore the possibility of lipid exchange as a regulatory mechanism of EPCR activity driven by the endothelially expressed secretory group V phospholipase A(2) (sPLA(2)-V). We identified phosphatidylcholine (PCh) as the major phospholipid bound to human soluble EPCR (sEPCR). PCh in EPCR could be exchanged for lysophosphatidylcholine (lysoPCh) and platelet activating factor (PAF). Remarkably, lysoPCh and PAF impaired the protein C binding ability of sEPCR. Inhibition of sPLA(2)-V, responsible for lysoPCh and PAF generation, improved APC binding to endothelial cells. EPCR-dependent protein C activation and APC antiapoptotic effect were thus significantly enhanced. In contrast, endothelial cell supplementation with sPLA(2)-V inhibited both APC generation and its antiapoptotic effects. We conclude that APC generation and function can be modulated by changes in phospholipid occupancy of its endothelial cell receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antigens, CD / chemistry*
  • Antigens, CD / metabolism*
  • Chromatography, Thin Layer
  • Endothelial Cells / metabolism
  • Endothelial Protein C Receptor
  • Enzyme Activation / physiology
  • Flow Cytometry
  • Group V Phospholipases A2 / metabolism*
  • Humans
  • Immunohistochemistry
  • Lysophosphatidylcholines / chemistry*
  • Lysophosphatidylcholines / metabolism
  • Mass Spectrometry
  • Mice
  • Platelet Activating Factor / chemistry*
  • Platelet Activating Factor / metabolism
  • Protein C / metabolism*
  • Protein Structure, Tertiary
  • Receptors, Cell Surface / chemistry*
  • Receptors, Cell Surface / metabolism*
  • Spectrometry, Fluorescence

Substances

  • Antigens, CD
  • Endothelial Protein C Receptor
  • Lysophosphatidylcholines
  • PROCR protein, human
  • Platelet Activating Factor
  • Protein C
  • Receptors, Cell Surface
  • Group V Phospholipases A2