Lysophosphatidic Acid Receptors

Lysophosphatidic acid (LPA) receptors are a group of G-protein-coupled receptors that are currently divided into six subtypes: LPA1, LPA2, LPA3, LPA4, LPA5 and LPA6. They belong to a family of lysophospholipid receptors that include S1P receptors.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
4779 GRI 977143
Selective LPA2 receptor non-lipid agonist
3854 1-Oleoyl lysophosphatidic acid sodium salt
Endogenous agonist of LPA1 and LPA2

Antagonists

Cat No Product Name / Activity
4870 H2L 5765834
LPA1,3,5 antagonist
4878 H2L5186303
Potent and selective LPA2 receptor antagonist
5056 Ki 16425
LPA1 and LPA3 receptor antagonist
5913 Ro 6842262
Potent LPA1 antagonist
4708 TC LPA5 4
LPA5 receptor antagonist

Lysophosphatidic acid (LPA) receptors are a group of G-protein-coupled receptors that are currently divided into six subtypes: LPA1, LPA2, LPA3, LPA4, LPA5 and LPA6. They belong to a family of lysophospholipid receptors that include sphingosine 1-phosphate (S1P) receptors.

Originally identified as members of the endothelial differentiation gene (edg) family, the gene names for the LPA receptors have recently been updated to LPAR1-LPAR3, with LPAR4-LPAR6 also having been updated to reflect their main physiological ligand, lysophosphatidic acid.

LPA1, LPA2 and LPA3 receptors belong within the EDG family and are widely expressed. Whereas, LPA4 and LPA5 receptors are found within the P2Y gene cluster and expressed in low levels in many tissues but with high expression in the ovary and small intestine respectively. LPA6 has recently been identified and is expressed highly in leukocytes, small intestine and hair cells. Additional receptors have also been identified that may qualify as LPA7-LPA9 receptors based on their activation by LPA, although this is pending the publication of additional evidence concerning identity. LPA receptors regulate a broad range of cellular functions: cell proliferation and survival, migration and chemotaxis, cytoskeletal architecture, cell-cell-contacts and adhesion, Ca2+ homoeostasis and Ca2+-dependent functions. They have been implicated in development, regulation of the cardiovascular, immune and nervous systems, inflammation, atherosclerosis, neuropathic pain, fibrosis in the kidney and lung, as well as male infertility and cancer.

External sources of pharmacological information for Lysophosphatidic Acid Receptors :

    Literature for Lysophosphatidic Acid Receptors

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    LPA Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Lysophosphatidic Acid
    Receptor 1
    Human LPAR1 NM_057159 Q92633
    Mouse Lpar1 NM_172989 P61793
    Rat Lpar1 NM_053936 P61794
    Lysophosphatidic Acid
    Receptor 2
    Human LPAR2 NM_004720 Q9HBW0
    Mouse Lpar2 NM_020028 Q6P290
    Rat Lpar2 NM_001109109 NP_001102579
    Lysophosphatidic Acid
    Receptor 3
    Human LPAR3 NM_012152 Q9UBY5
    Mouse Lpar3 NM_022983 Q9EQ31
    Rat Lpar3 NM_023969 Q8K5E0
    Lysophosphatidic Acid
    Receptor 4
    Human LPAR4 NM_005296 Q99677
    Mouse Lpar4 NM_175271 Q8BLG2
    Rat Lpar4 NM_001106940 NP_001100410
    Lysophosphatidic Acid
    Receptor 5
    Human LPAR5 NM_020400 Q9H1C0
    Mouse Lpar5 NM_001163268 Q149R9
    Rat Lpar5 XM_001063300 XP_001063300
    Lysophosphatidic Acid
    Receptor 6
    Human LPAR6 NM_005767 P43657
    Mouse Lpar6 NM_175116 Q8BMC0
    Rat Lpar6 NM_001045843 Q4G072