Lysophospholipid Family Related Drug Discovery Products

The bioactive lipids known as lysophospholipids (LPs), which include lysophosphatidic acid (LPA), sphingosine 1-phospate (S1P), lysophosphatidylinositol (LPI), and lysophosphatidylserine (LysoPS), transmit signals through the particular GPCRs. These LPs and their receptors have been linked to both physiological and pathophysiological processes, including fibrosis, pain, cancer, inflammation, metabolic syndrome, bone formation, fertility, organismal development, and other effects on the majority of organ systems. These processes include autoimmune diseases, neurodegenerative diseases, and diseases of the nervous system. Novel small compounds that target LP receptors for a number of disorders have been made possible by developments in the field of LP receptors.

Fig.1. Lysophospholipid receptors.^1,2

Creative Biolabs offers a range of lysophospholipid family drug discovery assays and products in a timely and cost-effective manner:

Lysophospholipid GPCR Assays GPCR Assay Kits GPCR Cell Lines GPCR Membranes Membrane Protein Tools

Overview of Lysophospholipid Family

• LPA receptors

Cellular responses that depend on LPAR1 include cytoskeletal modification, cell motility, adhesion, and Ca²⁺ mobilization. LPAR1 binds to Gα_i/o, Gα_q/11, and Gα_12/13. LPAR2 links to several G-proteins, such as Gα_i/o, Gα_q/11, and Gα_12/13, and is linked to immunological function, brain development, cancer metastasis, cell migration, and cancer metastasis. LPAR3 favours unsaturated fatty acids found in 2-acyl-LPA and transmits signaling through Gα_i/o and Gα_q/11. Involved in neurite retraction, cell motility, cell aggregation and adhesion, osteoblast development, and blood and lymphatic channel creation, LPAR4 couples to Gα_s, Gα_si/o, Gα_q/11, and Gα_12/13. LPAR5 can bind to Gα_q/11 and Gα_12/13 and uses a non-Gα_s method to promote cAMP accumulation. LPAR5 controls the immune system and neuropathic pain.

• S1P receptors

S1PR1 links to Gα_i/o and promotes intracellular signaling, including activation of MAPK, small GTPase Rac, suppression of cyclic AMP buildup, intracellular Ca²⁺ rise, and probably additional signals. S1PR2 preferentially couples to various G-proteins, including Gα_i/o, Gα_q/11, and Gα_12/13, to activate Rho signaling. By preventing Rac activation, S1PR2 eliminates motility. To Gα_i/o, Gα_q/11, and Gα_12/13, S1PR3 pairings. Breast cancer, sepsis, and liver fibrosis are just a few of the illnesses that S1P-S1PR3 signaling may be related to. Gα_i/o and Gα_12/13 are the signaling transducers used by S1PR4. It is believed that this receptor, which is more prevalent in mature hematopoietic organs, encourages cell migration. S1PR5 can couple to Gα_i/o and Gα_12/13, but it may prefer to couple to Gα_12/13 given its shared functions in restricting cell migration and encouraging cell process retraction. S1PR5 is crucial for the differentiation of NK cells and lymphocyte trafficking.

Lysophospholipid Family Drug Discovery

LTB4 and cysteinylleukotriene release both encourage the recruitment of inflammatory cells and heighten the inflammatory response. Leukotriene receptors on vascular smooth muscle and endothelial cells also cause changes in the vascular wall's structure and function that are related to atherosclerosis. A quick exchange of information regarding atherosclerosis is made possible by the therapeutic application of leukotriene modifiers in the treatment of allergies and asthma at the moment. Leukotrienes have a role in atherosclerosis because they are locally formed within the atherosclerotic lesion and have strong pro-inflammatory effects when leukotriene receptors are activated in target cells.

References

1. Gaire, Bhakta Prasad, and Ji-Woong Choi. "Critical roles of lysophospholipid receptors in activation of neuroglia and their neuroinflammatory responses." International Journal of Molecular Sciences 22.15 (2021): 7864.
2. Distributed under Open Access License CC BY 4.0, without modification.