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Identification
- Summary
Phosphatidyl serine is a nutrient used in some supplement products.
- Brand Names
- EnBrace HR, EnLyte
- Generic Name
- Phosphatidyl serine
- DrugBank Accession Number
- DB00144
- Background
Phosphatidyl serine (PS) is a phospholipid nutrient found in fish, green leafy vegetables, soybeans and rice, and is essential for the normal functioning of neuronal cell membranes and activates Protein kinase C (PKC) which has been shown to be involved in memory function. In apoptosis, phosphatidyl serine is transferred to the outer leaflet of the plasma membrane. This is part of the process by which the cell is targeted for phagocytosis. PS has been shown to slow cognitive decline in animal models. PS has been investigated in a small number of double-blind placebo trials and has been shown to increase memory performance in the elderly. Because of the potentail cognitive benefits of phosphatidylserine, the substance is sold as a dietary supplement to people who believe they can benefit from an increased intake.
The dietary supplement was originally processed from bovine sources however Prion disease scares in the 1990s outlawed this process, and a soy-based alternative was adopted.
- Type
- Small Molecule
- Groups
- Investigational, Nutraceutical
- Structure
Structure for Phosphatidyl serine (DB00144)
- Weight
- Average: 792.089
Monoisotopic: 791.567634842 - Chemical Formula
- C42H82NO10P
- Synonyms
- Phosphatidyl serine
- Phosphatidylserine
- PS
Pharmacology
- Indication
Phosphatidylserine has demonstrated some usefulness in treating cognitive impairment, including Alzheimer's disease, age-associated memory impairment and some non-Alzheimer's dementias. More research is needed before phosphatidylserine can be indicated for immune enhancement or for reduction of exercise stress.
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Phosphatidylserine is indicated in the treatment of cognitive impairment, including Alzheimer's disease, age-associated memory impairment and some non-Alzheimer's dementias. Further research is required before phosphatidylserine can be indicated for immune enhancement or for reduction of exercise stress. Phosphatidylserine was first isolated from brain lipids called cephalins. The major cephalins are phosphatidylserine and phophatidylethanolamine. Phosphatidylserine is involved in signal transduction activity as well as being a basic structural component of biologic membranes.
- Mechanism of action
Cholinergic hypofunction is thought to account in part for the cognitive deficits found in Alzheimer's disease. The most commonly used drugs for the treatment of Alzheimer's disease are reversible acetylcholinesterase inhibitors. The rationale of these drugs is to increase acetylcholine levels in the brains of Alzheimer's patients, and they may be somewhat effective in some cases. Phosphatidylserine restores acetylcholine release in aging humans by maintaining an adequate supply of the molecule and is able to increase the availability of endogenous choline for de novo acetylcholine synthesis. The hippocampus of the brain is believed to be important for cognitive processes and is affected in those with Alzheimer's disease. The dendritic spines of pyramidal cells, the post-synaptic target of the excitatory input to the hippocampus, have been proposed as a substrate for information storage. Age-dependent dendritic spine loss in pyramidal neurons has been reported in the human brain, and the extent of synaptic loss appears to correlate with the degree of cognitive impairment. Phosphatidylserine treatment prevents the age-related reduction in dendritic spine density in rat hippocampus. Protein kinase C facilitation of acetylcholine release has been reported in rats. Phosphatidylserine was found to restore protein kinase C activity in aging rats. Stimulation of calcium uptake by brain synaptosomes and activation of protein kinase C are yet other speculative mechanisms of phosphatidylserine's putative cognition-enhancing action.
Target Actions Organism UPhosphatidylserine decarboxylase proenzyme, mitochondrial Not Available Humans UScavenger receptor class B member 1 Not Available Humans UProtein kinase C alpha type Not Available Humans UPhosphatidylserine synthase 1 Not Available Humans UDiacylglycerol kinase gamma Not Available Humans UDiacylglycerol kinase delta Not Available Humans UPhosphatidylserine synthase 2 Not Available Humans USphingomyelin phosphodiesterase 4 Not Available Humans USphingomyelin phosphodiesterase 3 Not Available Humans UPhospholipid-transporting ATPase IA Not Available Humans - Absorption
Absorbed in the small intestine.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Following absorption, lysophosphatidylserine is metabolized in intestinal mucosa cells, and its metabolites, which include some phosphatidylserine, enter the lymphatics draining the small intestine.
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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There are no reports of overdosage. LD50 in rats is more than 5g/kg, and in rabbits is more than 2g/kg.
- Pathways
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Products
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- LifeExtension PS Caps
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Oil Phosphatidyl serine (1.5 mg/15mg) + Coffee bean (1.5 mg/15mg) + Green tea leaf (2.25 mg/15mg) + Omega-3 fatty acids (2.25 mg/15mg) + Tyrosine (4.5 mg/15mg) Oil Cutaneous Shantou Youjia E-Commerce Co., Ltd. 2024-02-01 2024-12-31 US 
PramLyte Phosphatidyl serine (12 mg/1) + 1,2-docosahexanoyl-sn-glycero-3-phosphoserine calcium (6.4 mg/1) + 1,2-icosapentoyl-sn-glycero-3-phosphoserine calcium (800 ug/1) + Betaine (500 ug/1) + Citric acid monohydrate (1.83 mg/1) + Cobamamide (50 ug/1) + Cocarboxylase (25 ug/1) + Escitalopram oxalate (10 mg/1) + Ferrous cysteine glycinate (13.6 mg/1) + Flavin adenine dinucleotide (25 ug/1) + Folic acid (1 mg/1) + Leucovorin (2.5 mg/1) + Levomefolate magnesium (7 mg/1) + Magnesium ascorbate (24 mg/1) + NADH (25 ug/1) + Pyridoxal phosphate (25 ug/1) + Sodium citrate (3.67 mg/1) + Zinc ascorbate (1 mg/1) Kit Oral Allegis Pharmaceuticals, LLC 2015-09-11 2016-01-04 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image EnBrace HR Phosphatidyl serine (12 mg/1) + 1,2-docosahexanoyl-sn-glycero-3-phosphoserine calcium (6.4 mg/1) + 1,2-icosapentoyl-sn-glycero-3-phosphoserine calcium (800 ug/1) + Betaine (500 ug/1) + Cobamamide (50 ug/1) + Cocarboxylase (25 ug/1) + Ferrous cysteine glycinate (13.6 mg/1) + Flavin adenine dinucleotide (25 ug/1) + Folic acid (1 mg/1) + Magnesium L-threonate (1 mg/1) + Leucovorin (2.5 mg/1) + Levomefolate magnesium (5.23 mg/1) + Magnesium ascorbate (24 mg/1) + NADH (25 ug/1) + Pyridoxal phosphate (25 ug/1) + Zinc ascorbate (1 mg/1) Capsule, delayed release pellets Oral Jaymac Pharmaceuticals Llc 2011-08-12 Not applicable US PaxLyte Phosphatidyl serine (12 mg/1) + 1,2-docosahexanoyl-sn-glycero-3-phosphoserine calcium (6.4 mg/1) + 1,2-icosapentoyl-sn-glycero-3-phosphoserine calcium (800 ug/1) + Betaine (500 mg/1) + Citric acid monohydrate (1.83 mg/1) + Cobamamide (50 ug/1) + Cocarboxylase (25 ug/1) + Ferrous cysteine glycinate (13.6 mg/1) + Flavin adenine dinucleotide (025 ug/1) + Folic acid (1 mg/1) + Magnesium L-threonate (1 mg/1) + Leucovorin (2.5 mg/1) + Levomefolate magnesium (7 mg/1) + Magnesium ascorbate (24 mg/1) + NADH (25 ug/1) + Pyridoxal phosphate (25 ug/1) + Sodium citrate (1.83 mg/1) + Zinc ascorbate (1 mg/1) Capsule Oral Jaymac Pharmaceuticals Llc 2024-08-01 Not applicable US
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 394XK0IH40
- CAS number
- 1446756-47-3
- InChI Key
- TZCPCKNHXULUIY-RGULYWFUSA-N
- InChI
- InChI=1S/C42H82NO10P/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-40(44)50-35-38(36-51-54(48,49)52-37-39(43)42(46)47)53-41(45)34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2/h38-39H,3-37,43H2,1-2H3,(H,46,47)(H,48,49)/t38-,39+/m1/s1
- IUPAC Name
- (2S)-2-amino-3-({[(2R)-2,3-bis(octadecanoyloxy)propoxy](hydroxy)phosphoryl}oxy)propanoic acid
- SMILES
- CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCCCCCCCCCCCC
References
- Synthesis Reference
Lorenzo De Ferra, Pietro Massardo, Oreste Piccolo, Stefano Servi, "Process for the industrial preparation of phosphatidylserine." U.S. Patent US5700668, issued January, 1992.
US5700668- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0012378
- PubChem Compound
- 6323481
- PubChem Substance
- 46505650
- ChemSpider
- 7826046
- 89959
- ChEBI
- 84519
- ChEMBL
- CHEMBL4297669
- ZINC
- ZINC000085588270
- PharmGKB
- PA164768860
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- P5S
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Phosphatidylserine
- PDB Entries
- 4b2z / 6i3y / 6lcp / 6lcr / 6lkn / 6sp2 / 6tt7 / 6vp0 / 6zzx / 6zzy … show 44 more
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data4 Withdrawn Treatment Menstrual Related Mood Disorder / Premenstrual Dysphoric Disorder (PMDD) / Premenstrual Syndrome (PMS) / Premenstrual tension with edema 1 somestatus stop reason just information to hide 2 Completed Treatment Attention Deficit Hyperactivity Disorder (ADHD) 1 somestatus stop reason just information to hide 1 Completed Treatment Rectal Adenocarcinoma 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Professional Co.
- Dosage Forms
Form Route Strength Capsule, liquid filled Oral Capsule, delayed release pellets Oral Capsule Oral Oil Cutaneous Kit Oral - Prices
Unit description Cost Unit Phosphatidylserine 40% powder 13.2USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP -3.5 Not Available - Predicted Properties
Property Value Source Water Solubility 6.74e-05 mg/mL ALOGPS logP 4.95 ALOGPS logP 11.27 Chemaxon logS -7.1 ALOGPS pKa (Strongest Acidic) 1.47 Chemaxon pKa (Strongest Basic) 9.38 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 171.68 Å2 Chemaxon Rotatable Bond Count 44 Chemaxon Refractivity 215.24 m3·mol-1 Chemaxon Polarizability 96.63 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.6612 Blood Brain Barrier + 0.5475 Caco-2 permeable - 0.666 P-glycoprotein substrate Non-substrate 0.5358 P-glycoprotein inhibitor I Non-inhibitor 0.7716 P-glycoprotein inhibitor II Non-inhibitor 0.9679 Renal organic cation transporter Non-inhibitor 0.9512 CYP450 2C9 substrate Non-substrate 0.9229 CYP450 2D6 substrate Non-substrate 0.8056 CYP450 3A4 substrate Non-substrate 0.6063 CYP450 1A2 substrate Non-inhibitor 0.7648 CYP450 2C9 inhibitor Non-inhibitor 0.8731 CYP450 2D6 inhibitor Non-inhibitor 0.8662 CYP450 2C19 inhibitor Non-inhibitor 0.7588 CYP450 3A4 inhibitor Non-inhibitor 0.7248 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9716 Ames test Non AMES toxic 0.7626 Carcinogenicity Non-carcinogens 0.7671 Biodegradation Not ready biodegradable 0.7036 Rat acute toxicity 2.1996 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9279 hERG inhibition (predictor II) Non-inhibitor 0.7921
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 371.8473394 predictedDarkChem Lite v0.1.0 [M-H]- 277.88324 predictedDeepCCS 1.0 (2019) [M+H]+ 370.9222394 predictedDarkChem Lite v0.1.0 [M+H]+ 280.27933 predictedDeepCCS 1.0 (2019) [M+Na]+ 370.9544394 predictedDarkChem Lite v0.1.0 [M+Na]+ 286.19263 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalyzes the formation of phosphatidylethanolamine (PtdEtn) from phosphatidylserine (PtdSer) (PubMed:30488656, PubMed:30858161). Plays a central role in phospholipid metabolism and in the interorganelle trafficking of phosphatidylserine. May be involved in lipid droplet biogenesis at the endoplasmic reticulum membrane (By similarity)
- Specific Function
- phosphatidylserine decarboxylase activity
- Gene Name
- PISD
- Uniprot ID
- Q9UG56
- Uniprot Name
- Phosphatidylserine decarboxylase proenzyme, mitochondrial
- Molecular Weight
- 46671.34 Da
References
- Wu WI, Voelker DR: Reconstitution of phosphatidylserine transport from chemically defined donor membranes to phosphatidylserine decarboxylase 2 implicates specific lipid domains in the process. J Biol Chem. 2004 Feb 20;279(8):6635-42. Epub 2003 Dec 4. [Article]
- Burgermeister M, Birner-Grunberger R, Heyn M, Daum G: Contribution of different biosynthetic pathways to species selectivity of aminoglycerophospholipids assembled into mitochondrial membranes of the yeast Saccharomyces cerevisiae. Biochim Biophys Acta. 2004 Nov 8;1686(1-2):148-60. [Article]
- Burgermeister M, Birner-Grunberger R, Nebauer R, Daum G: Contribution of different pathways to the supply of phosphatidylethanolamine and phosphatidylcholine to mitochondrial membranes of the yeast Saccharomyces cerevisiae. Biochim Biophys Acta. 2004 Nov 8;1686(1-2):161-8. [Article]
- Roggero R, Zufferey R, Minca M, Richier E, Calas M, Vial H, Ben Mamoun C: Unraveling the mode of action of the antimalarial choline analog G25 in Plasmodium falciparum and Saccharomyces cerevisiae. Antimicrob Agents Chemother. 2004 Aug;48(8):2816-24. [Article]
- Voelker DR: Protein and lipid motifs regulate phosphatidylserine traffic in yeast. Biochem Soc Trans. 2005 Nov;33(Pt 5):1141-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Receptor for different ligands such as phospholipids, cholesterol ester, lipoproteins, phosphatidylserine and apoptotic cells (PubMed:12016218, PubMed:12519372, PubMed:21226579). Receptor for HDL, mediating selective uptake of cholesteryl ether and HDL-dependent cholesterol efflux (PubMed:26965621). Also facilitates the flux of free and esterified cholesterol between the cell surface and apoB-containing lipoproteins and modified lipoproteins, although less efficiently than HDL. May be involved in the phagocytosis of apoptotic cells, via its phosphatidylserine binding activity (PubMed:12016218)
- Specific Function
- 1-phosphatidylinositol binding
- Gene Name
- SCARB1
- Uniprot ID
- Q8WTV0
- Uniprot Name
- Scavenger receptor class B member 1
- Molecular Weight
- 60877.385 Da
References
- Yan X, Poelstra K, Scherphof GL, Kamps JA: A role for scavenger receptor B-I in selective transfer of rhodamine-PE from liposomes to cells. Biochem Biophys Res Commun. 2004 Dec 17;325(3):908-14. [Article]
- Yancey PG, Kawashiri MA, Moore R, Glick JM, Williams DL, Connelly MA, Rader DJ, Rothblat GH: In vivo modulation of HDL phospholipid has opposing effects on SR-BI- and ABCA1-mediated cholesterol efflux. J Lipid Res. 2004 Feb;45(2):337-46. Epub 2003 Nov 1. [Article]
- Nakagawa A, Shiratsuchi A, Tsuda K, Nakanishi Y: In vivo analysis of phagocytosis of apoptotic cells by testicular Sertoli cells. Mol Reprod Dev. 2005 Jun;71(2):166-77. [Article]
- Zhang J, Fujii S, Wu Z, Hashioka S, Tanaka Y, Shiratsuchi A, Nakanishi Y, Nakanishi H: Involvement of COX-1 and up-regulated prostaglandin E synthases in phosphatidylserine liposome-induced prostaglandin E2 production by microglia. J Neuroimmunol. 2006 Mar;172(1-2):112-20. Epub 2005 Dec 20. [Article]
- Osada Y, Shiratsuchi A, Nakanishi Y: Involvement of mitogen-activated protein kinases in class B scavenger receptor type I-induced phagocytosis of apoptotic cells. Exp Cell Res. 2006 Jun 10;312(10):1820-30. Epub 2006 Mar 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that is involved in positive and negative regulation of cell proliferation, apoptosis, differentiation, migration and adhesion, tumorigenesis, cardiac hypertrophy, angiogenesis, platelet function and inflammation, by directly phosphorylating targets such as RAF1, BCL2, CSPG4, TNNT2/CTNT, or activating signaling cascade involving MAPK1/3 (ERK1/2) and RAP1GAP. Involved in cell proliferation and cell growth arrest by positive and negative regulation of the cell cycle. Can promote cell growth by phosphorylating and activating RAF1, which mediates the activation of the MAPK/ERK signaling cascade, and/or by up-regulating CDKN1A, which facilitates active cyclin-dependent kinase (CDK) complex formation in glioma cells. In intestinal cells stimulated by the phorbol ester PMA, can trigger a cell cycle arrest program which is associated with the accumulation of the hyper-phosphorylated growth-suppressive form of RB1 and induction of the CDK inhibitors CDKN1A and CDKN1B. Exhibits anti-apoptotic function in glioma cells and protects them from apoptosis by suppressing the p53/TP53-mediated activation of IGFBP3, and in leukemia cells mediates anti-apoptotic action by phosphorylating BCL2. During macrophage differentiation induced by macrophage colony-stimulating factor (CSF1), is translocated to the nucleus and is associated with macrophage development. After wounding, translocates from focal contacts to lamellipodia and participates in the modulation of desmosomal adhesion. Plays a role in cell motility by phosphorylating CSPG4, which induces association of CSPG4 with extensive lamellipodia at the cell periphery and polarization of the cell accompanied by increases in cell motility. During chemokine-induced CD4(+) T cell migration, phosphorylates CDC42-guanine exchange factor DOCK8 resulting in its dissociation from LRCH1 and the activation of GTPase CDC42 (PubMed:28028151). Is highly expressed in a number of cancer cells where it can act as a tumor promoter and is implicated in malignant phenotypes of several tumors such as gliomas and breast cancers. Negatively regulates myocardial contractility and positively regulates angiogenesis, platelet aggregation and thrombus formation in arteries. Mediates hypertrophic growth of neonatal cardiomyocytes, in part through a MAPK1/3 (ERK1/2)-dependent signaling pathway, and upon PMA treatment, is required to induce cardiomyocyte hypertrophy up to heart failure and death, by increasing protein synthesis, protein-DNA ratio and cell surface area. Regulates cardiomyocyte function by phosphorylating cardiac troponin T (TNNT2/CTNT), which induces significant reduction in actomyosin ATPase activity, myofilament calcium sensitivity and myocardial contractility. In angiogenesis, is required for full endothelial cell migration, adhesion to vitronectin (VTN), and vascular endothelial growth factor A (VEGFA)-dependent regulation of kinase activation and vascular tube formation. Involved in the stabilization of VEGFA mRNA at post-transcriptional level and mediates VEGFA-induced cell proliferation. In the regulation of calcium-induced platelet aggregation, mediates signals from the CD36/GP4 receptor for granule release, and activates the integrin heterodimer ITGA2B-ITGB3 through the RAP1GAP pathway for adhesion. During response to lipopolysaccharides (LPS), may regulate selective LPS-induced macrophage functions involved in host defense and inflammation. But in some inflammatory responses, may negatively regulate NF-kappa-B-induced genes, through IL1A-dependent induction of NF-kappa-B inhibitor alpha (NFKBIA/IKBA). Upon stimulation with 12-O-tetradecanoylphorbol-13-acetate (TPA), phosphorylates EIF4G1, which modulates EIF4G1 binding to MKNK1 and may be involved in the regulation of EIF4E phosphorylation. Phosphorylates KIT, leading to inhibition of KIT activity. Phosphorylates ATF2 which promotes cooperation between ATF2 and JUN, activating transcription. Phosphorylates SOCS2 at 'Ser-52' facilitating its ubiquitination and proteasomal degradation (By similarity). Phosphorylates KLHL3 in response to angiotensin II signaling, decreasing the interaction between KLHL3 and WNK4 (PubMed:25313067). Phosphorylates and activates LRRK1, which phosphorylates RAB proteins involved in intracellular trafficking (PubMed:36040231)
- Specific Function
- ATP binding
- Gene Name
- PRKCA
- Uniprot ID
- P17252
- Uniprot Name
- Protein kinase C alpha type
- Molecular Weight
- 76749.445 Da
References
- Yu D, Kazanietz MG, Harvey RG, Penning TM: Polycyclic aromatic hydrocarbon o-quinones inhibit the activity of the catalytic fragment of protein kinase C. Biochemistry. 2002 Oct 1;41(39):11888-94. [Article]
- Rodriguez-Alfaro JA, Gomez-Fernandez JC, Corbalan-Garcia S: Role of the lysine-rich cluster of the C2 domain in the phosphatidylserine-dependent activation of PKCalpha. J Mol Biol. 2004 Jan 23;335(4):1117-29. [Article]
- Lopez-Andreo MJ, Torrecillas A, Conesa-Zamora P, Corbalan-Garcia S, Gomez-Fernandez JC: Retinoic acid as a modulator of the activity of protein kinase Calpha. Biochemistry. 2005 Aug 30;44(34):11353-60. [Article]
- Corbin JA, Evans JH, Landgraf KE, Falke JJ: Mechanism of specific membrane targeting by C2 domains: localized pools of target lipids enhance Ca2+ affinity. Biochemistry. 2007 Apr 10;46(14):4322-36. Epub 2007 Mar 17. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalyzes a base-exchange reaction in which the polar head group of phosphatidylethanolamine (PE) or phosphatidylcholine (PC) is replaced by L-serine (PubMed:19014349, PubMed:24241535). Catalyzes mainly the conversion of phosphatidylcholine (PubMed:19014349, PubMed:24241535). Also converts, in vitro and to a lesser extent, phosphatidylethanolamine (PubMed:19014349, PubMed:24241535)
- Specific Function
- L-serine-phosphatidylcholine phosphatidyltransferase activity
- Gene Name
- PTDSS1
- Uniprot ID
- P48651
- Uniprot Name
- Phosphatidylserine synthase 1
- Molecular Weight
- 55527.18 Da
References
- Kuge O, Nishijima M: Biosynthetic regulation and intracellular transport of phosphatidylserine in mammalian cells. J Biochem. 2003 Apr;133(4):397-403. [Article]
- Kuge O, Hasegawa K, Ohsawa T, Saito K, Nishijima M: Purification and characterization of Chinese hamster phosphatidylserine synthase 2. J Biol Chem. 2003 Oct 24;278(43):42692-8. Epub 2003 Aug 11. [Article]
- Ohsawa T, Nishijima M, Kuge O: Functional analysis of Chinese hamster phosphatidylserine synthase 1 through systematic alanine mutagenesis. Biochem J. 2004 Aug 1;381(Pt 3):853-9. [Article]
- Steenbergen R, Nanowski TS, Nelson R, Young SG, Vance JE: Phospholipid homeostasis in phosphatidylserine synthase-2-deficient mice. Biochim Biophys Acta. 2006 Mar;1761(3):313-23. Epub 2006 Mar 31. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Diacylglycerol kinase that converts diacylglycerol/DAG into phosphatidic acid/phosphatidate/PA and regulates the respective levels of these two bioactive lipids (PubMed:8034597). Thereby, acts as a central switch between the signaling pathways activated by these second messengers with different cellular targets and opposite effects in numerous biological processes (By similarity). Has no apparent specificity with regard to the acyl compositions of diacylglycerol (PubMed:8034597). Specifically expressed in the cerebellum where it controls the level of diacylglycerol which in turn regulates the activity of protein kinase C gamma. Through protein kinase C gamma, indirectly regulates the dendritic development of Purkinje cells, cerebellar long term depression and ultimately cerebellar motor coordination (By similarity)
- Specific Function
- ATP binding
- Gene Name
- DGKG
- Uniprot ID
- P49619
- Uniprot Name
- Diacylglycerol kinase gamma
- Molecular Weight
- 89123.27 Da
References
- Yamaguchi Y, Shirai Y, Matsubara T, Sanse K, Kuriyama M, Oshiro N, Yoshino K, Yonezawa K, Ono Y, Saito N: Phosphorylation and up-regulation of diacylglycerol kinase gamma via its interaction with protein kinase C gamma. J Biol Chem. 2006 Oct 20;281(42):31627-37. Epub 2006 Aug 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Diacylglycerol kinase that converts diacylglycerol/DAG into phosphatidic acid/phosphatidate/PA and regulates the respective levels of these two bioactive lipids (PubMed:12200442, PubMed:23949095). Thereby, acts as a central switch between the signaling pathways activated by these second messengers with different cellular targets and opposite effects in numerous biological processes (Probable). By controlling the levels of diacylglycerol, regulates for instance the PKC and EGF receptor signaling pathways and plays a crucial role during development (By similarity). May also regulate clathrin-dependent endocytosis (PubMed:17880279)
- Specific Function
- ATP binding
- Gene Name
- DGKD
- Uniprot ID
- Q16760
- Uniprot Name
- Diacylglycerol kinase delta
- Molecular Weight
- 134524.235 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Bregoli L, Baldassare JJ, Raben DM: Nuclear diacylglycerol kinase-theta is activated in response to alpha-thrombin. J Biol Chem. 2001 Jun 29;276(26):23288-95. Epub 2001 Apr 17. [Article]
- Sakane F, Imai S, Kai M, Wada I, Kanoh H: Molecular cloning of a novel diacylglycerol kinase isozyme with a pleckstrin homology domain and a C-terminal tail similar to those of the EPH family of protein-tyrosine kinases. J Biol Chem. 1996 Apr 5;271(14):8394-401. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalyzes a base-exchange reaction in which the polar head group of phosphatidylethanolamine (PE) or phosphatidylcholine (PC) is replaced by L-serine (PubMed:19014349). Catalyzes the conversion of phosphatatidylethanolamine and does not act on phosphatidylcholine (PubMed:19014349). Can utilize both phosphatidylethanolamine (PE) plasmalogen and diacyl PE as substrate and the latter is six times better utilized, indicating the importance of an ester linkage at the sn-1 position (By similarity). Although it shows no sn-1 fatty acyl preference, exhibits significant preference towards docosahexaenoic acid (22:6n-3) compared with 18:1 or 20:4 at the sn-2 position (By similarity)
- Specific Function
- CDP-diacylglycerol-serine O-phosphatidyltransferase activity
- Gene Name
- PTDSS2
- Uniprot ID
- Q9BVG9
- Uniprot Name
- Phosphatidylserine synthase 2
- Molecular Weight
- 56252.55 Da
References
- Bergo MO, Gavino BJ, Steenbergen R, Sturbois B, Parlow AF, Sanan DA, Skarnes WC, Vance JE, Young SG: Defining the importance of phosphatidylserine synthase 2 in mice. J Biol Chem. 2002 Dec 6;277(49):47701-8. Epub 2002 Oct 1. [Article]
- Vance JE, Vance DE: Phospholipid biosynthesis in mammalian cells. Biochem Cell Biol. 2004 Feb;82(1):113-28. [Article]
- Dygas A, Baranska J, Santella L: Ca2+-dependent phosphatidylserine synthesis in immature and mature starfish oocytes. Acta Biochim Pol. 2003;50(2):377-87. [Article]
- Grandmaison PA, Nanowski TS, Vance JE: Externalization of phosphatidylserine during apoptosis does not specifically require either isoform of phosphatidylserine synthase. Biochim Biophys Acta. 2004 Feb 27;1636(1):1-11. [Article]
- Wen Z, Kim HY: Inhibition of phosphatidylserine biosynthesis in developing rat brain by maternal exposure to ethanol. J Neurosci Res. 2007 May 15;85(7):1568-78. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalyzes the hydrolysis of membrane sphingomyelin to form phosphorylcholine and ceramide (PubMed:16517606, PubMed:25180167). It has a relevant role in the homeostasis of membrane sphingolipids, thereby influencing membrane integrity, and endoplasmic reticulum organization and function (PubMed:31495489). May sensitize cells to DNA damage-induced apoptosis (PubMed:18505924). In skeletal muscle, mediates TNF-stimulated oxidant production (By similarity)
- Specific Function
- metal ion binding
- Gene Name
- SMPD4
- Uniprot ID
- Q9NXE4
- Uniprot Name
- Sphingomyelin phosphodiesterase 4
- Molecular Weight
- 97808.955 Da
References
- Krut O, Wiegmann K, Kashkar H, Yazdanpanah B, Kronke M: Novel tumor necrosis factor-responsive mammalian neutral sphingomyelinase-3 is a C-tail-anchored protein. J Biol Chem. 2006 May 12;281(19):13784-93. Epub 2006 Mar 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalyzes the hydrolysis of sphingomyelin to form ceramide and phosphocholine. Ceramide mediates numerous cellular functions, such as apoptosis and growth arrest, and is capable of regulating these 2 cellular events independently. Also hydrolyzes sphingosylphosphocholine. Regulates the cell cycle by acting as a growth suppressor in confluent cells. Probably acts as a regulator of postnatal development and participates in bone and dentin mineralization (PubMed:10823942, PubMed:14741383, PubMed:15051724). Binds to anionic phospholipids (APLs) such as phosphatidylserine (PS) and phosphatidic acid (PA) that modulate enzymatic activity and subcellular location. May be involved in IL-1-beta-induced JNK activation in hepatocytes (By similarity). May act as a mediator in transcriptional regulation of NOS2/iNOS via the NF-kappa-B activation under inflammatory conditions (By similarity)
- Specific Function
- identical protein binding
- Gene Name
- SMPD3
- Uniprot ID
- Q9NY59
- Uniprot Name
- Sphingomyelin phosphodiesterase 3
- Molecular Weight
- 71080.1 Da
References
- Krut O, Wiegmann K, Kashkar H, Yazdanpanah B, Kronke M: Novel tumor necrosis factor-responsive mammalian neutral sphingomyelinase-3 is a C-tail-anchored protein. J Biol Chem. 2006 May 12;281(19):13784-93. Epub 2006 Mar 3. [Article]
- Marchesini N, Luberto C, Hannun YA: Biochemical properties of mammalian neutral sphingomyelinase 2 and its role in sphingolipid metabolism. J Biol Chem. 2003 Apr 18;278(16):13775-83. Epub 2003 Feb 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Catalytic component of a P4-ATPase flippase complex which catalyzes the hydrolysis of ATP coupled to the transport of aminophospholipids from the outer to the inner leaflet of various membranes and ensures the maintenance of asymmetric distribution of phospholipids (PubMed:31416931). Phospholipid translocation seems also to be implicated in vesicle formation and in uptake of lipid signaling molecules. In vitro, its ATPase activity is selectively and stereospecifically stimulated by phosphatidylserine (PS) (PubMed:31416931). The flippase complex ATP8A1:TMEM30A seems to play a role in regulation of cell migration probably involving flippase-mediated translocation of phosphatidylethanolamine (PE) at the cell membrane (By similarity). Acts as aminophospholipid translocase at the cell membrane in neuronal cells (By similarity)
- Specific Function
- ATP binding
- Gene Name
- ATP8A1
- Uniprot ID
- Q9Y2Q0
- Uniprot Name
- Phospholipid-transporting ATPase IA
- Molecular Weight
- 131368.215 Da
References
- Bettache N, Baisamy L, Baghdiguian S, Payrastre B, Mangeat P, Bienvenue A: Mechanical constraint imposed on plasma membrane through transverse phospholipid imbalance induces reversible actin polymerization via phosphoinositide 3-kinase activation. J Cell Sci. 2003 Jun 1;116(Pt 11):2277-84. Epub 2003 Apr 15. [Article]
- Wolfs JL, Comfurius P, Rasmussen JT, Keuren JF, Lindhout T, Zwaal RF, Bevers EM: Activated scramblase and inhibited aminophospholipid translocase cause phosphatidylserine exposure in a distinct platelet fraction. Cell Mol Life Sci. 2005 Jul;62(13):1514-25. [Article]
- Mandal D, Mazumder A, Das P, Kundu M, Basu J: Fas-, caspase 8-, and caspase 3-dependent signaling regulates the activity of the aminophospholipid translocase and phosphatidylserine externalization in human erythrocytes. J Biol Chem. 2005 Nov 25;280(47):39460-7. Epub 2005 Sep 22. [Article]
- Paterson JK, Renkema K, Burden L, Halleck MS, Schlegel RA, Williamson P, Daleke DL: Lipid specific activation of the murine P4-ATPase Atp8a1 (ATPase II). Biochemistry. 2006 Apr 25;45(16):5367-76. [Article]
Drug created at June 13, 2005 13:24 / Updated at August 02, 2024 07:22