Lysophosphatidylinositols, from Cell Membrane Constituents to GPR55 Ligands

Trends Pharmacol Sci. 2018 Jun;39(6):586-604. doi: 10.1016/j.tips.2018.02.011. Epub 2018 Mar 24.

Abstract

Lysophosphatidylinositols (LPIs) are membrane constituents that alter the properties of said membranes. However, recent data showing that the once orphan receptor, GPR55, can act as a receptor for LPIs has sparked a renewed interest in LPIs as bioactive lipids. As evidence supporting the importance of LPIs and/or GPR55 is continuously accumulating and because LPI levels are altered in a number of pathologies such as obesity and cancer, the coming years should bring new, exciting discoveries to this field. In this review, we discuss the recent work on LPIs and on their molecular target, the GPR55 receptor. First, we summarize the metabolism of LPIs before outlining the cellular pathways activated by GPR55. Then, we review the actions of LPIs and GPR55 that could have potential pharmacological or therapeutic applications in several pathophysiological settings, such as cancer, obesity, pain, and inflammation.

Publication types

  • Review

MeSH terms

  • Allosteric Regulation
  • Animals
  • Cell Membrane / metabolism*
  • Drug Design*
  • Humans
  • Ligands
  • Lysophospholipids / biosynthesis
  • Lysophospholipids / chemistry
  • Lysophospholipids / metabolism*
  • Protein Binding
  • Receptors, Cannabinoid
  • Receptors, G-Protein-Coupled* / agonists
  • Receptors, G-Protein-Coupled* / antagonists & inhibitors
  • Receptors, G-Protein-Coupled* / genetics

Substances

  • GPR55 protein, human
  • Ligands
  • Lysophospholipids
  • Receptors, Cannabinoid
  • Receptors, G-Protein-Coupled
  • lysophosphatidylinositol