The interaction of plasminogen activator inhibitor 1 with plasminogen activators (tissue-type and urokinase-type) and fibrin: localization of interaction sites and physiologic relevance

Blood. 1991 Jul 15;78(2):401-9.

Abstract

Plasminogen activator inhibitor 1 (PAI-1), an essential regulatory protein of the fibrinolytic system, harbors interaction sites for plasminogen activators (tissue-type [t-PA] and urokinase-type [u-PA]) and for fibrin. In this study, anti-PAI-1 monoclonal antibodies (MoAbs) were used to identify interaction sites of PAI-1 with these components. The binding sites of 18 different MoAbs were established and are located on five distinct "linear" areas of PAI-1. MoAbs, binding to two distinct areas of PAI-1, are able to prevent the inhibition of t-PA by PAI-1. In addition, two interaction sites for fibrin were identified on PAI-1. The area located between amino acids 110 and 145 of PAI-1 contains a binding site for both components and its significance is discussed in the context of the t-PA inhibition by fibrin-bound PAI-1. Subsequently, the MoAbs were used to assess the role of platelet-PAI-1 in clot-lysis. An in vitro clot-lysis system was used to demonstrate that clot-lysis resistance is dependent on the presence of activated platelets and that PAI-1 is a major determinant for lysis-resistance. We propose that, upon activation of platelets, PAI-1 is fixed within the clot by binding to fibrin and retains its full capacity to inhibit t-PA and u-PA.

MeSH terms

  • Antibodies, Monoclonal
  • Binding Sites
  • Chromosome Deletion
  • Enzyme Precursors / metabolism
  • Enzyme Precursors / physiology
  • Epitopes / analysis
  • Fibrin / metabolism
  • Fibrinolysis
  • Humans
  • Plasminogen Activators / metabolism*
  • Plasminogen Activators / physiology
  • Plasminogen Inactivators / metabolism*
  • Tissue Plasminogen Activator / metabolism*
  • Tissue Plasminogen Activator / physiology
  • Urokinase-Type Plasminogen Activator / metabolism*
  • Urokinase-Type Plasminogen Activator / physiology

Substances

  • Antibodies, Monoclonal
  • Enzyme Precursors
  • Epitopes
  • Plasminogen Inactivators
  • Fibrin
  • Plasminogen Activators
  • Tissue Plasminogen Activator
  • Urokinase-Type Plasminogen Activator