Lysophospholipid (LPA) receptors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Lysophosphatidic acid (LPA) receptors (nomenclature as agreed by NC-IUPHAR Subcommittee on Lysophospholipid Receptors; [8]) are activated by the endogenous phospholipid metabolite LPA. The first receptor, LPA1, was identified as ventricular zone gene-1 (vzg-1), leading to deorphanisation of members of the endothelial differentiation gene (edg) family as other LPA receptors along with sphingosine 1-phosphate (S1P) receptors. Additional LPA receptor GPCRs were later identified. Gene names have been codified as LPAR1, etc. to reflect the receptor function of proteins. The identified receptors can account for most, although not all, LPA-induced phenomena in the literature, indicating that a majority of LPA-dependent phenomena are receptor-mediated. Radioligand binding has been conducted in heterologous expression systems using [3H]LPA (e.g. [3]). In native systems, analysis of binding data is complicated by metabolism and high levels of nonspecific binding, and therefore the relationship between recombinant and endogenously expressed receptors is unclear. Targeted deletion of LPA receptors has clarified signalling pathways and identified physiological and pathophysiological roles. Independent validation by multiple groups has been reported in the peer-reviewed literature for all six LPA receptors described in the tables, including further validation using a distinct read-out via a novel TGFα “shedding” assay [7]. LPA has also been described to be an agonist at other orphan GPCRs (PSP24, GPR87 and GPR35), as well as at the nuclear hormone PPARγ receptors [14,16], although the physiological significance of these observations remain unclear.

Receptors

LPA1 receptor Show summary » More detailed page

LPA2 receptor Show summary » More detailed page

LPA3 receptor Show summary » More detailed page

LPA4 receptor Show summary » More detailed page

LPA5 receptor Show summary » More detailed page

LPA6 receptor Show summary » More detailed page

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Lysophospholipid (LPA) receptors. Accessed on 23/11/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=36.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.