Monday, September 25, 2023

Significance & Physiological Role of Tissue Factor Pathway Inhibitor (TFPI)

  • Tissue Factor Pathway Inhibitor (TFPI) is located

    • On Endothelial Cells (ECs)
    • On Monocytes
    • In Platelets 
    • In plasma 

  • Bulk of TFPI is associated with ECs

    • Measurement of low TFPI in plasma doesn’t mean TFPI deficiency 
    • TFPI associated with ECs → 4X in TFPI upon Heparin injection
    • Most of circulating TFPI is bound to lipoproteins & the C terminals are variably degraded  

  • Physiological Role 

    • TFPI inhibits FVIIa in a FXa-dependent manner
    • TFPI binds to & directly inhibits TF-FVIIa-FXa complex → So, it effectively halts TF initiated activation of coagulation but only after sufficient FXa has been generated to propagate coagulation
    • Plasma TFPI has reduced anticoagulant activity
      • So, likely not very important anticoagulant role in vivo

  • Therapeutic Role 

    • TFPI binds to Heparan Sulphate on EC surface
    • UFH or LMWH displace this bound TFPI → This released TFPI contributes to antithrombotic activities of these drugs

  • Isoforms of TFPI

    • Two isoforms exist 
      • TFPIα
      • TFPIβ 
    • TFPIα has 3 Kunitz type protease inhibitory domains → K1, K2, K3 
      • K1 domain inhibits FVIIa in a FXa dependent manner 
      • K2 directly binds & inhibits FXa
    • Protein S (PS) acts as cofactor in the formation of TFPI-FXa complex

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