Homers regulate calcium entry and aggregation in human platelets: a role for Homers in the association between STIM1 and Orai1

Biochem J. 2012 Jul 1;445(1):29-38. doi: 10.1042/BJ20120471.

Abstract

Homer is a family of cytoplasmic adaptor proteins that play different roles in cell function, including the regulation of G-protein-coupled receptors. These proteins contain an Ena (Enabled)/VASP (vasodilator-stimulated phosphoprotein) homology 1 domain that binds to the PPXXF sequence motif, which is present in different Ca²⁺-handling proteins such as IP3 (inositol 1,4,5-trisphosphate) receptors and TRPC (transient receptor potential canonical) channels. In the present study we show evidence for a role of Homer proteins in the STIM1 (stromal interaction molecule 1)-Orai1 association, as well as in the TRPC1-IP3RII (type II IP3 receptor) interaction, which might be of relevance in platelet function. Treatment of human platelets with thapsigargin or thrombin results in a Ca²⁺-independent association of Homer1 with TRPC1 and IP3RII. In addition, thapsigargin and thrombin enhanced the association of Homer1 with STIM1 and Orai1 in a Ca²⁺-dependent manner. Interference with Homer function by introduction of the synthetic PPKKFR peptide into cells, which emulates the proline-rich sequences of the PPXXF motif, reduced STIM1-Orai1 and TRPC1- IP3RII associations, as compared with the introduction of the inactive PPKKRR peptide. The PPKKFR peptide attenuates thrombin-evoked Ca²⁺ entry and the maintenance of thapsigargin-induced store-operated Ca²⁺ entry. Finally, the PPKKFR peptide attenuated thrombin-induced platelet aggregation. The findings of the present study support an important role for Homer proteins in thrombin-stimulated platelet function, which is likely to be mediated by the support of agonist-induced Ca²⁺ entry.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Blood Platelets / drug effects
  • Blood Platelets / metabolism*
  • Blotting, Western
  • Calcium Channels / metabolism*
  • Calcium Signaling / drug effects
  • Calcium Signaling / physiology*
  • Carrier Proteins / metabolism*
  • Cell Proliferation / drug effects
  • Enzyme Inhibitors / pharmacology
  • Homer Scaffolding Proteins
  • Humans
  • Immunoprecipitation
  • Inositol 1,4,5-Trisphosphate / metabolism
  • Inositol 1,4,5-Trisphosphate Receptors / metabolism*
  • Membrane Proteins / metabolism*
  • Neoplasm Proteins / metabolism*
  • ORAI1 Protein
  • Peptide Fragments / metabolism
  • Platelet Aggregation / drug effects
  • Protein Binding
  • Stromal Interaction Molecule 1
  • TRPC Cation Channels / metabolism*
  • Thapsigargin / pharmacology

Substances

  • Calcium Channels
  • Carrier Proteins
  • Enzyme Inhibitors
  • HOMER1 protein, human
  • Homer Scaffolding Proteins
  • Inositol 1,4,5-Trisphosphate Receptors
  • Membrane Proteins
  • Neoplasm Proteins
  • ORAI1 Protein
  • ORAI1 protein, human
  • Peptide Fragments
  • STIM1 protein, human
  • Stromal Interaction Molecule 1
  • TRPC Cation Channels
  • transient receptor potential cation channel, subfamily C, member 1
  • Thapsigargin
  • Inositol 1,4,5-Trisphosphate