Lysophospholipid
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Lysophospholipid
The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eleven LPL receptors, each encoded by a separate gene. These LPL receptor genes are also sometimes referred to as "Edg" (an acronym for endothelial differentiation gene). Ligands The ligands for LPL-R group are the lysophospholipid extracellular signaling molecules, lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P). Origin of name The term ''lysophospholipid'' (LPL) refers to any phospholipid that is missing one of its two O- acyl chains. Thus, LPLs have a free alcohol in either the sn-1 or the sn-2 position. The prefix 'lyso-' comes from the fact that lysophospholipids were originally found to be hemolytic, however it is now used to refer generally to phospholipids missing an acyl chain. LPLs are usually the result of phospholipase A-type enzymatic activity on regular phospho ...
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Lipid Signaling
Lipid signaling, broadly defined, refers to any biological cell signaling event involving a lipid messenger that binds a protein target, such as a receptor (biochemistry), receptor, kinase or phosphatase, which in turn mediate the effects of these lipids on specific cellular responses. Lipid signaling is thought to be qualitatively different from other classical signaling paradigms (such as monoamine neurotransmission) because lipids can freely molecular diffusion, diffuse through Cell membrane, membranes (''see osmosis''). One consequence of this is that lipid messengers cannot be stored in Vesicle (biology), vesicles prior to release and so are often biosynthesis, biosynthesized "on demand" at their intended site of action. As such, many lipid signaling molecules cannot circulate freely in solution but, rather, exist bound to special carrier proteins in serous fluid, serum. Sphingolipid second messengers Ceramide Ceramide (Cer) can be generated by the breakdown of sphingom ...
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LPAR1
Lysophosphatidic acid receptor 1 also known as LPA1 is a protein that in humans is encoded by the ''LPAR1'' gene. LPA1 is a G protein-coupled receptor that binds the lipid signaling molecule lysophosphatidic acid (LPA). Function The integral membrane protein encoded by this gene is a lysophosphatidic acid (LPA) receptor from a group known as Endothelial differentiation gene, EDG receptors. These receptors are members of the G protein-coupled receptor superfamily. Utilized by LPA for cell signaling, EDG receptors mediate diverse biologic functions, including proliferation, platelet aggregation, smooth muscle contraction, inhibition of neuroblastoma cell differentiation, chemotaxis, and tumor cell invasion. Alternative splicing of this gene has been observed and two transcript variants have been described, each encoding identical proteins. An alternate translation start codon has been identified, which results in isoforms differing in the N-terminal extracellular tail. In additio ...
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S1PR5
Sphingosine-1-phosphate receptor 5 also known as S1PR5 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P5. Agonists * A-971432 * Sphingosine 1-phosphate receptor agonists: a patent review (2010-2012) Evolution Paralogues for S1PR5 Gene * S1PR1 * S1PR3 * S1PR2 * S1PR4 * LPAR1 * LPAR2 * GPR3 * LPAR3 * GPR12 * CNR1 * GPR6 * CNR2 * MC4R * MC3R * MC5R * GPR119 * MC1R * MC2R See also * Lysophospholipid receptor The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eleven LPL receptor (biochemistry), receptors, each encode ... References Further reading * * * * * * * * * * * * * External links * * G protein-coupled receptors {{transmembranereceptor-stub ...
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S1PR4
Sphingosine-1-phosphate receptor 4 also known as S1PR4 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P4. Function This gene is a member of the endothelial differentiation, G-protein-coupled (EDG) receptor gene family. EDG receptors bind lysophospholipids or lysosphingolipids as ligands, and are involved in cell signalling in many different cell types. This EDG receptor gene is intronless and is specifically expressed in the lymphoid tissue. Evolution Paralogues to S1PR4 Gene * S1PR5 * S1PR3 * S1PR1 * S1PR2 * LPAR2 * LPAR1 * LPAR3 * CNR1 * GPR6 * CNR2 * GPR3 * GPR12 * MC4R * MC5R * MC3R * MC2R * MC1R * GPR119 See also * Lysophospholipid receptor The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eleven L ...
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S1PR3
Sphingosine-1-phosphate receptor 3 also known as ''S1PR3'' is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P3. Function This gene encodes a member of the EDG family of receptors, which are G protein-coupled receptors. This protein has been identified as a functional receptor for sphingosine 1-phosphate and likely contributes to the regulation of angiogenesis and vascular endothelial cell function. Evolution Paralogues to S1PR3 Gene * S1PR1 * S1PR5 * S1PR2 * S1PR4 * LPAR1 * LPAR3 * LPAR2 * CNR1 * MC5R * GPR6 * GPR12 * MC4R * CNR2 * GPR3 * MC3R * MC2R * GPR119 * MC1R See also * Lysophospholipid receptor The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eleven LPL receptor (biochemistry), receptors, each ...
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S1PR2
Sphingosine-1-phosphate receptor 2, also known as S1PR2 or S1P2, is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Function This protein participates in sphingosine 1-phosphate-induced cell proliferation, survival, and transcriptional activation. It has also been shown to interact with Nogo-A (RTN4), an neurite outgrowth inhibitor. S1PR2 is expressed in neuronal and vascular cells and is crucial for the migration and growth of developing and injured neuronal and vascular system. Evolution Paralogues * S1PR1 * S1PR3 * S1PR5 * S1PR4 * LPAR2 * LPAR1 * LPAR3 * CNR1 * GPR6 * MC3R * GPR12 * GPR3 * MC4R * MC1R * CNR2 * MC5R * MC2R * GPR119 See also * Lysophospholipid receptor The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eleven LPL receptor (bioc ...
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S1PR1
Sphingosine-1-phosphate receptor 1 (S1P receptor 1 or S1PR1), also known as endothelial differentiation gene 1 (EDG1) is a protein that in humans is encoded by the ''S1PR1'' gene. S1PR1 is a G-protein-coupled receptor which binds the bioactive signaling molecule sphingosine 1-phosphate (S1P). S1PR1 belongs to a sphingosine-1-phosphate receptor subfamily comprising five members (S1PR1-5). S1PR1 was originally identified as an abundant transcript in endothelial cells and it has an important role in regulating endothelial cell cytoskeletal structure, migration, capillary-like network formation and vascular maturation. In addition, S1PR1 signaling is important in the regulation of lymphocyte maturation, migration and trafficking. Structure S1PR1 like the other members of the GPCR family is composed of seven-transmembrane helices arranged in a structurally conserved bundle. Like other GPCRs, in the extracellular region S1PR1 is composed of three loops: ECL1 between helices II an ...
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LPAR2
Lysophosphatidic acid receptor 2 also known as LPA2 is a protein that in humans is encoded by the ''LPAR2'' gene. LPA2 is a G protein-coupled receptor that binds the lipid signaling molecule lysophosphatidic acid (LPA). Function This gene encodes a member of family I of the G protein-coupled receptors, as well as the EDG family of proteins. This protein functions as a lysophosphatidic acid (LPA) receptor and contributes to Ca2+ mobilization, a critical cellular response to LPA in cells, through association with Gi and Gq proteins. Interactions LPAR2 has been shown to interact with TRIP6. Evolution Paralogues Source: * LPAR1 * LPAR3 * S1PR1 * S1PR5 * S1PR4 * S1PR2 * S1PR3 * GPR6 * GPR3 * GPR12 * MC4R * MC5R * CNR1 * MC3R * CNR2 * MC1R * GPR119 * MC2R See also * Lysophospholipid receptor The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In ...
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Lysophosphatidic Acid
A lysophosphatidic acid (LPA) is a phospholipid derivative that can act as a signaling molecule. Function LPA acts as a potent mitogen due to its activation of three high-affinity G-protein-coupled receptors called LPAR1, LPAR2, and LPAR3 (also known as EDG2, EDG4, and EDG7). Additional, newly identified LPA receptors include LPAR4 (P2RY9, GPR23), LPAR5 (GPR92) and LPAR6 (P2RY5, GPR87). Clinical significance Because of its ability to stimulate cell proliferation, aberrant LPA-signaling has been linked to cancer in numerous ways. Dysregulation of autotaxin or the LPA receptors can lead to hyperproliferation, which may contribute to oncogenesis and metastasis. LPA may be the cause of pruritus (itching) in individuals with cholestatic (impaired bile flow) diseases. GTPase activation Downstream of LPA receptor activation, the small GTPase Rho can be activated, subsequently activating Rho kinase. This can lead to the formation of stress fibers and cell migration through t ...
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LPAR3
Lysophosphatidic acid receptor 3 also known as LPA3 is a protein in humans that is encoded by the ''LPAR3'' gene. LPA3 is a G protein-coupled receptor that binds the lipid signaling molecule lysophosphatidic acid (LPA). Function This gene encodes a member of the G protein-coupled receptor family, as well as the EDG family of proteins. This protein functions as a cellular receptor for lysophosphatidic acid and mediates lysophosphatidic acid-evoked calcium mobilization. This receptor couples predominantly to G(q/11) alpha proteins. Evolution Paralogues Source: * LPAR1 * LPAR2 * S1PR1 * S1PR3 * S1PR4 * S1PR2 * S1PR5 * CNR1 * GPR3 * MC5R * GPR6 * GPR12 * MC4R * CNR2 * MC3R * MC1R * MC2R * GPR119 See also * Lysophospholipid receptor The lysophospholipid receptor (LPL-R) group are members of the G protein-coupled receptor family of integral membrane proteins that are important for lipid signaling. In humans, there are eleven LPL receptor (biochemistry), receptors, eac ...
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Gintonin
Gintonin is a glycolipoprotein fraction isolated from ''Panax ginseng''. The non-saponin ingredient was designated as gintonin, where ''gin'' was derived from ginseng, ''ton'' from the tonic effects of ginseng, and ''in'' from protein. The main component of gintonin is a complex of lysophosphatidic acids (LPA) and ginseng proteins such as ginseng major latex-like protein151 (GLP151) and ginseng ribonuclease-like storage protein. GLP151 is a first plant-derived LPA binding protein as one of Bet v 1 superfamily. GLP151 has a LPA binding domain on H147 and H148 at C-terminal. These two histidine residues bind to phosphate group of LPA. Biological action Gintonin is believed to act by delivering LPA to lysophospholipid receptors, which are high affinity and selective target receptors. In animal cell cultures, gintonin induces a2+transients via activation of the said receptor. One Korean study claims that gintonin is orally active in rodents and shows anti-Alzheimer's disease eff ...
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