Lysophospholipid Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
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. (Gaire & Choi, 2021)
Creative Biolabs offers a range of lysophospholipid family drug discovery assays and products in a timely and cost-effective manner:
Overview of Lysophospholipid Family
- LPA receptors
Cellular responses that depend on LPAR1 include cytoskeletal modification, cell motility, adhesion, and Ca2+ mobilization. LPAR1 binds to Gαi/o, Gαq/11, and Gα12/13. LPAR2 links to several G-proteins, such as Gαi/o, Gαq/11, and Gα12/13, 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 Gαi/o and Gαq/11. Involved in neurite retraction, cell motility, cell aggregation and adhesion, osteoblast development, and blood and lymphatic channel creation, LPAR4 couples to Gαs, Gαsi/o, Gαq/11, and Gα12/13. LPAR5 can bind to Gαq/11 and Gα12/13 and uses a non-Gαs method to promote cAMP accumulation. LPAR5 controls the immune system and neuropathic pain.
Fig.2 Generation and degradation of bioactive LPA. (Zu Heringdorf & Jakobs, 2007)
- S1P receptors
S1PR1 links to Gαi/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 Gαi/o, Gαq/11, and Gα12/13, to activate Rho signaling. By preventing Rac activation, S1PR2 eliminates motility. To Gαi/o, Gαq/11, and Gα12/13, S1PR3 pairings. Breast cancer, sepsis, and liver fibrosis are just a few of the illnesses that S1P-S1PR3 signaling may be related to. Gαi/o and Gα12/13 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 Gαi/o and Gα12/13, but it may prefer to couple to Gα12/13 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.
Fig.3 S1P receptors drug discovery. (Kihara, 2015)
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
- 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.
- Zu Heringdorf, D.M.; Jakobs, K.H. Lysophospholipid receptors: signaling, pharmacology and regulation by lysophospholipid metabolism. Biochimica et Biophysica Acta (BBA)-Biomembranes. 2007, 1768(4): 923-940.
- Kihara, Y.; et al. Lysophospholipid receptors in drug discovery. Experimental cell research. 2015, 333(2): 171-177.
