ReviewReceptors for acylethanolamides—GPR55 and GPR119
Section snippets
Acylethanolamides
Acylethanolamides or fatty acid ethanolamides are lipid substances widely distributed in the body, present both in brain and various peripheral tissues, most notably in the gastrointestinal tract [1]. They are thought to be generated from a membrane phospholipid precursor, N-acylphosphatidylethanolamine (NAPE) by phospholipase d-mediated cleavage [2], although additional, parallel enzymatic pathways have also been identified [3], [4]. NAPE has been recently identified as a hormone-like anorexic
The structure of GPR55
The cloning of the human GPR55 was originally reported in 1999, when it was described as a classical intronless GPCR that maps to chromosome 2 and consists of 319 amino acids. Philogenetically, GPR55 belongs to the δ (purine) cluster of the rhodopsin family that comprises receptors for adenosine and uridine nucleotides and also contains some orphan receptors [25], [26]. It displays limited amino acid sequence homology with GPR23 (30%), P2Y5 (29%), GPR35 (27%) and CCR4 (23%), homologies with CB1
Structure of GPR119
The human orphan receptor GPR119 was identified through a bioinformatics approach [26]. Its sequence was found to align with the earlier reported hGPCR2 receptor [59] and it is present in other mammalian species [26], [60]. The 335 amino acid hGPR119 protein is encoded by an intronless gene located on chromosome X [26], [59]. Philogenetically, GPR119 has been assigned to the MECA (melanocortin; endothelial differentiation gene; cannabinoid; adenosine) receptor cluster, which designates
References (75)
- et al.
Role of acylethanolamides in the gastrointestinal tract with special reference to food intake and energy balance
Best Pract Res Clin Endocrinol Metab
(2009) - et al.
Anandamide biosynthesis catalyzed by the phosphodiesterase GDE1 and detection of glycerophospho-N-acyl ethanolamine precursors in mouse brain
J Biol Chem
(2008) - et al.
N-acylphosphatidylethanolamine, a gut-derived circulating factor induced by fat ingestion, inhibits food intake
Cell
(2008) - et al.
Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors
Biochem Pharmacol
(1995) - et al.
2-Arachidonoylglycerol: a possible endogenous cannabinoid receptor ligand in brain
Biochem Biophys Res Commun
(1995) - et al.
Evidence for novel cannabinoid receptors
Pharmacol Ther
(2005) The enigmatic pharmacology of GPR55
Trends Pharmacol Sci
(2009)- et al.
In silico patent searching reveals a new cannabinoid receptor
Trends Pharmacol Sci
(2006) - et al.
Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents
Cell Metab
(2006) - et al.
Cellular and molecular biology of orphan G protein-coupled receptors
Int Rev Cytol
(2006)
Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives
FEBS Lett
Identification and cloning of three novel human G protein-coupled receptor genes GPR52, PsiGPR53 and GPR55: GPR55 is extensively expressed in human brain
Brain Res Mol Brain Res
Identification of GPR55 as a lysophosphatidylinositol receptor
Biochem Biophys Res Commun
Biological activities and metabolism of the lysophosphoinositides and glycerophosphoinositols
Biochim Biophys Acta
EDHF: bringing the concepts together
Trends Pharmacol Sci
Atypical cannabinoid stimulates endothelial cell migration via a Gi/Go-coupled receptor distinct from CB1, CB2 or EDG-1
Eur J Pharmacol
2-Arachidonylglyceryl ether and abnormal cannabidiol-induced vascular smooth muscle relaxation in rabbit pulmonary arteries via receptor-pertussis toxin sensitive G proteins-ERK1/2 signaling
Eur J Pharmacol
Cannabinoid receptor homo- and heterodimerization
Life Sci
The putative cannabinoid receptor GPR55 plays a role in mechanical hyperalgesia associated with inflammatory and neuropathic pain
Pain
Identification of G protein-coupled receptor genes from the human genome sequence
FEBS Lett
Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor
Biochem Biophys Res Commun
Expression and distribution of Gpr119 in the pancreatic islets of mice and rats: predominant localization in pancreatic polypeptide-secreting PP-cells
Biochem Biophys Res Commun
Glucose sensing in L cells: a primary cell study
Cell Metab
The lipid messenger OEA links dietary fat intake to satiety
Cell Metab
Oleoylethanolamide stimulates lipolysis by activating the nuclear receptor peroxisome proliferator-activated receptor alpha (PPAR-alpha)
J Biol Chem
Oleoylethanolamide exerts partial and dose-dependent neuroprotection of substantia nigra dopamine neurons
Neuropharmacology
Analgesic properties of oleoylethanolamide (OEA) in visceral and inflammatory pain
Pain
Formation and inactivation of endogenous cannabinoid anandamide in central neurons
Nature
A biosynthetic pathway for anandamide
Proc Natl Acad Sci USA
Isolation and structure of a brain constituent that binds to the cannabinoid receptor
Science
Structure of a cannabinoid receptor and functional expression of the cloned cDNA
Nature
Molecular characterization of a peripheral receptor for cannabinoids
Nature
Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide
Nature
Novel cannabinoid receptors
Br J Pharmacol
GPR55 and the vascular receptors for cannabinoids
Br J Pharmacol
GPR55 as a new cannabinoid receptor: still a long way to prove it
Chem Biol Drug Des
Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-alpha
Nature
Cited by (0)
- 1
Current address: Keufbeuren Hospital, Keufbeuren, Germany.