P2Y1 and P2Y12 receptor heterodimerisation: from recombinant systems to native detection

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Abstract

Purinergic P2Y1 and P2Y12 receptors belong to the class A family of transmembrane G‐protein coupled receptors (GPCRs) and have been demonstrated to exist as homodimers and oligomers and form heterodimers with other GPCRs. P2Y12 and protease‐activated receptor 4 (PAR4) were recently reported to form a heterodimer with implications in receptor trafficking and signalling. Our unpublished studies suggest that hP2Y1 and hP2Y12 heterodimerise; therefore, the aim of this study was to investigate the functional relevance of receptor interaction, firstly in recombinant systems and then natively in microglial cells. hP2Y1 and hP2Y12 receptor heterodimersation impacted ADP‐mediated internalisation when both receptors are overexpressed in tSA201 cells. Co‐localisation studies in BV‐2 cells suggest that the location of receptor interaction may differ depending upon the cell types explored. Further work is under way to investigate these differences.
Original languageEnglish
Pages (from-to)3049
Number of pages1
JournalBritish Journal of Pharmacology
Volume176
Issue number16
Early online date9 Jul 2019
DOIs
Publication statusPublished - 1 Aug 2019
EventPharmacology 2018 - QEII Centre, London, United Kingdom
Duration: 18 Dec 201820 Dec 2018
https://www.bps.ac.uk/news-events/events/2018/december/pharmacology-2018

Keywords

  • P2Y1 receptors
  • P2Y12 receptors
  • G‐protein coupled receptors (GPCRs)
  • heterodimersation

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