Lysophospholipid GPCR Assays
Background of Lysophospholipid Receptors
Lysophospholipids (LPs) are a family of phospholipids that are involved in a broad range of biological processes through GPCRs. lysophosphatidic acid (LPA), sphingosine 1-phosphate (S1P), lysophosphatidylinositol (LPI), and lysophosphatidylserine (LysoPS) are classical members of transduce signals through their specific cell-surface G protein-coupled receptors. The lysophospholipid receptor (LPL-R) group is important for lipid signaling and has served as the target for immunomodulation in transplant therapy.
Fig.1. IPF pathology and accessed mechanisms for an LPA1 antagonist. (Kihara, 2015)
Distribution and Function of Lysophospholipid Receptors
Studies have shown that LPA1, LPA2, and LPA3 receptors are widely expressed. Whereas, high expression of LPA4 and LPA5 receptors can be detected in the ovary and small intestine respectively. They can regulate cellular Ca2+ homeostasis and the cytoskeleton, proliferation and survival, migration and adhesion.
Subtypes and Mechanisms of Lysophospholipid Receptors
Currently, lysophospholipid receptors contain six LPA (LPA1–6) and five S1P receptors (S1P1–5). They are associated with the development and regulation of the cardiovascular, immune and nervous systems, inflammation, arteriosclerosis, and cancer.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| Lysophosphatidic acid receptor 1 | LPAR1 |
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| Lysophosphatidic acid receptor 2 | LPAR2 |
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| Lysophosphatidic acid receptor 3 | LPAR3 |
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| Lysophosphatidic acid receptor 4 | LPAR4 |
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| Lysophosphatidic acid receptor 5 | LPAR5 |
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| Lysophosphatidic acid receptor 6 | LPAR6 |
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| Sphingosine-1-phosphate receptor 1 | S1PR1 |
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| Sphingosine-1-phosphate receptor 2 | S1PR2 |
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| Sphingosine-1-phosphate receptor 3 | S1PR3 |
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| Sphingosine-1-phosphate receptor 4 | S1PR4 |
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| Sphingosine-1-phosphate receptor 5 | S1PR5 |
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Assay List of Lysophospholipid Receptors
Creative Biolabs can provide a range of assays of lysophospholipid receptors. You can choose the assay in the list or contact us for more information:
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| IP1 Assay | ||||
| S01YF-1122-KX570 | Magic™ Human LPAR3 In Vitro IP1 Assay | U2OS | IP1 Assay | |
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| IP1 Assay | ||||
| S01YF-1122-KX571 | Magic™ Human LPAR5 In Vitro IP1 Assay | CHO-K1 | IP1 Assay | |
Published Data
| Paper Title | Critical Roles of Lysophospholipid Receptors in Activation of Neuroglia and Their Neuroinflammatory Responses |
| Journal | International Journal of Molecular Sciences |
| Published | 2021 |
| Abstract | Activation of microglia and/or astrocytes are important pathogenic mediators that contribute to neuroinflammation and secondary brain injury in a variety of diseases of the central nervous system (CNS). Therefore, the activation of glial cells and their neuroinflammatory responses can be used to treat neuroinflammatory diseases. Furthermore, receptor-mediated lysophospholipid signaling plays a key role in the pathogenesis of several neurological diseases. Studies have shown that lysophospholipid receptors may affect glial cell activation and influence glial cell activation in various pathogenesis. This article provides information on the role of S1P and LPA receptors in neuroinflammatory responses in central nervous system disorders. |
| Result |
S1P and LPA receptors are expressed on both microglia and astrocytes and regulate neuroinflammatory responses through activation of the cells. Studies have shown that the expression of these two receptors is upregulated in CNS pathogenesis. It has been reported that S1P1, S1P2, S1P3, S1P5, LPA1, and LPA5 can promote the activation of microglia and/or astrocytes and their neuroinflammatory responses. However, the role of other receptors such as S1P4, LPA2, LPA4, and LPA6 remains unclear. In recent years, research on LPA and S1P receptors has mainly focused on cerebral ischemia and MS, and more attention will be paid to other CNS diseases such as PD, AD, and Huntington's disease in the future. Furthermore, the development of new modulators of S1P and LPA receptor subtypes may serve as a therapeutic option for CNS diseases.
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Fig.2. Either pharmacological or genetic approaches have been employed to identify the roles of S1P and LPA receptors in glial activation under neuroinflammatory conditions. (Gaire & Choi)
References
- Kihara, Y.; et al. Lysophospholipid receptors in drug discovery. Experimental cell research. 2015, 333(2): 171-177.
- Gaire, B.P.; Choi, J.W. Critical roles of lysophospholipid receptors in activation of neuroglia and their neuroinflammatory responses. International Journal of Molecular Sciences. 2021, 22(15): 7864.
