Platelet factor 4 binds to low-density lipoprotein receptors and disrupts the endocytic machinery, resulting in retention of low-density lipoprotein on the cell surface

Blood. 2002 May 15;99(10):3613-22. doi: 10.1182/blood.v99.10.3613.

Abstract

The influence of platelets on the cellular metabolism of atherogenic lipoproteins has not been characterized in detail. Therefore, we investigated the effect of platelet factor 4 (PF4), a cationic protein released in high concentration by activated platelets, on the uptake and degradation of low-density lipoprotein (LDL) via the LDL receptor (LDL-R). LDL-R-dependent binding, internalization, and degradation of LDL by cultured cells were inhibited 50%, 80%, and 80%, respectively, on addition of PF4. PF4 bound specifically to the ligand-binding domain of recombinant soluble LDL-R (half-maximal binding 0.5 microg/mL PF4) and partially (approximately 50%) inhibited the binding of LDL. Inhibition of internalization and degradation by PF4 required the presence of cell-associated proteoglycans, primarily those rich in chondroitin sulfate. PF4 variants with impaired heparin binding lacked the capacity to inhibit LDL. PF4, soluble LDL-R, and LDL formed ternary complexes with cell-surface proteoglycans. PF4 induced the retention of LDL/LDL-R complexes on the surface of human fibroblasts in multimolecular clusters unassociated with coated pits, as assessed by immuno-electron microscopy. These studies demonstrate that PF4 inhibits the catabolism of LDL in vitro in part by competing for binding to LDL-R, by promoting interactions with cell-associated chondroitin sulfate proteoglycans, and by disrupting the normal endocytic trafficking of LDL/LDL-R complexes. Retention of LDL on cell surfaces may facilitate proatherogenic modifications and support an expanded role for platelets in the pathogenesis of atherosclerosis.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding, Competitive
  • CHO Cells
  • Cell Membrane / metabolism
  • Cell Membrane / ultrastructure
  • Cells, Cultured
  • Cricetinae
  • Dose-Response Relationship, Drug
  • Endocytosis*
  • Fibroblasts / metabolism
  • Fibroblasts / ultrastructure
  • Humans
  • Lipoproteins, LDL / metabolism*
  • Lipoproteins, LDL / ultrastructure
  • Platelet Factor 4 / metabolism*
  • Platelet Factor 4 / pharmacology*
  • Proteoglycans / physiology
  • Receptors, LDL / antagonists & inhibitors*
  • Receptors, LDL / metabolism
  • Receptors, LDL / ultrastructure

Substances

  • Lipoproteins, LDL
  • Proteoglycans
  • Receptors, LDL
  • Platelet Factor 4