Proteins > Phospholipase A2, membrane associated
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Phospholipase A2, membrane associated
A phospholipase A2, membrane associated that is encoded in the genome of human. [PRO:DNx, UniProtKB:P14555]
Synonyms
EC 3.1.1.4;
GIIC sPLA2;
Group IIA phospholipase A2;
Non-pancreatic secretory phospholipase A2;
NPS-PLA2;
Phosphatidylcholine 2-acylhydrolase 2A
Research
Bioassay Publications (22)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (4.55) | 18.7374 |
| 1990's | 6 (27.27) | 18.2507 |
| 2000's | 9 (40.91) | 29.6817 |
| 2010's | 5 (22.73) | 24.3611 |
| 2020's | 1 (4.55) | 2.80 |
Compounds (15)
Drugs with Inhibition Measurements
Drugs with Other Measurements
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Substrate-Specific Inhibition Constants for Phospholipase AJournal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase AACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
Discovery of AZD2716: A Novel Secreted Phospholipase AACS medicinal chemistry letters, , Oct-13, Volume: 7, Issue:10, 2016
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
The first potent inhibitor of mammalian group X secreted phospholipase A2: elucidation of sites for enhanced binding.Journal of medicinal chemistry, , May-18, Volume: 49, Issue:10, 2006
Carbocyclic[g]indole inhibitors of human nonpancreatic s-PLA2.Journal of medicinal chemistry, , Feb-10, Volume: 48, Issue:3, 2005
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
Design of new potent and selective secretory phospholipase A(2) inhibitors. 6-Synthesis, structure-activity relationships and molecular modelling of 1-substituted-4-[4,5-dihydro-1,2,4-(4H)-oxadiazol-5-one-3-yl(methyl)]-functionalized aryl piperazin/one/diBioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Inhibition of secreted phospholipase A2. 4-glycerol derivatives of 4,5-dihydro-3-(4-tetradecyloxybenzyl)-1,2,4-4H-oxadiazol-5-one with broad activities.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 2. Indole-3-acetamides with additional functionality.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
New sesquiterpene derivatives from the sponge Dysidea species with a selective inhibitor profile against human phospholipase A2 and other leukocyte functions.Journal of natural products, , Volume: 64, Issue:5, 2001
A new cacospongionolide inhibitor of human secretory phospholipase A2 from the Tyrrhenian sponge Fasciospongia cavernosa and absolute configuration of cacospongionolides.Journal of natural products, , Volume: 61, Issue:7, 1998
Synthesis and comparison of the antiinflammatory activity of manoalide and cacospongionolide B analogues.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Synthesis and phospholipase A2 inhibitory activity of thielocin B3 derivatives.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| phospholipase A2 activity | molecular function | Catalysis of the reaction: a 1,2-diacyl-sn-glycero-3-phospholipid + H2O = 1-acyl-sn-glycero-3-phospholipid + a fatty acid. This reaction removes the fatty acid attached to the sn2-position. Substrates include phosphatidylcholine, phosphatidylethanolamine, choline plasmalogen and phosphatides. [RHEA:15801] |
| phospholipid binding | molecular function | Binding to a phospholipid, a class of lipids containing phosphoric acid as a mono- or diester. [ISBN:0198506732] |
| calcium-dependent phospholipase A2 activity | molecular function | Catalysis of the reaction: phosphatidylcholine + H2O = 1-acylglycerophosphocholine + a carboxylate. This reaction requires Ca2+. [EC:3.1.1.4] |
| calcium ion binding | molecular function | Binding to a calcium ion (Ca2+). [GOC:ai] |
Located In
This protein is located in 9 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| mitochondrial outer membrane | cellular component | The outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| secretory granule | cellular component | A small subcellular vesicle, surrounded by a membrane, that is formed from the Golgi apparatus and contains a highly concentrated protein destined for secretion. Secretory granules move towards the periphery of the cell and upon stimulation, their membranes fuse with the cell membrane, and their protein load is exteriorized. Processing of the contained protein may take place in secretory granules. [GOC:mah, ISBN:0198506732] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Involved In
This protein is involved in 16 target(s):
| Target | Category | Definition |
|---|
| phospholipid metabolic process | biological process | The chemical reactions and pathways involving phospholipids, any lipid containing phosphoric acid as a mono- or diester. [ISBN:0198506732] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| positive regulation of macrophage derived foam cell differentiation | biological process | Any process that increases the rate, frequency or extent of macrophage derived foam cell differentiation. Macrophage derived foam cell differentiation is the process in which a macrophage acquires the specialized features of a foam cell. A foam cell is a type of cell containing lipids in small vacuoles and typically seen in atherosclerotic lesions, as well as other conditions. [GOC:add, GOC:dph, GOC:tb] |
| lipid catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of lipids, compounds soluble in an organic solvent but not, or sparingly, in an aqueous solvent. [GOC:go_curators] |
| killing of cells of another organism | biological process | Any process in an organism that results in the killing of cells of another organism, including in some cases the death of the other organism. Killing here refers to the induction of death in one cell by another cell, not cell-autonomous death due to internal or other environmental conditions. [GOC:add] |
| low-density lipoprotein particle remodeling | biological process | The acquisition, loss or modification of a protein or lipid within a low-density lipoprotein particle, including the hydrolysis of triglyceride by hepatic lipase, with the subsequent loss of free fatty acid, and the transfer of cholesterol esters from LDL to a triglyceride-rich lipoprotein particle by cholesteryl ester transfer protein (CETP), with the simultaneous transfer of triglyceride to LDL. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:rl] |
| intestinal stem cell homeostasis | biological process | Any biological process involved in the maintenance of the steady-state number of intestinal stem cells within a population of cells. [GOC:nhn, PMID:22042863, PMID:22608824] |
| phosphatidylethanolamine metabolic process | biological process | The chemical reactions and pathways involving phosphatidylethanolamine, any of a class of glycerophospholipids in which a phosphatidyl group is esterified to the hydroxyl group of ethanolamine. It is a major structural phospholipid in mammalian systems. It tends to be more abundant than phosphatidylcholine in the internal membranes of the cell and is an abundant component of prokaryotic membranes. [GOC:curators, ISBN:0198506732] |
| phosphatidylcholine metabolic process | biological process | The chemical reactions and pathways involving phosphatidylcholines, any of a class of glycerophospholipids in which the phosphatidyl group is esterified to the hydroxyl group of choline. They are important constituents of cell membranes. [ISBN:0198506732] |
| phosphatidic acid metabolic process | biological process | The chemical reactions and pathways involving phosphatidic acid, any derivative of glycerol phosphate in which both the remaining hydroxyl groups of the glycerol moiety are esterified with fatty acids. [ISBN:0198506732] |
| arachidonic acid secretion | biological process | The controlled release of arachidonic acid from a cell or a tissue. [GOC:ai] |
| positive regulation of inflammatory response | biological process | Any process that activates or increases the frequency, rate or extent of the inflammatory response. [GOC:ai] |
| defense response to Gram-positive bacterium | biological process | Reactions triggered in response to the presence of a Gram-positive bacterium that act to protect the cell or organism. [GOC:ai] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
| regulation of neutrophil activation | biological process | Any process that modulates the frequency, rate or extent of neutrophil activation. [GOC:TermGenie, PMID:17588661] |
| negative regulation of T cell proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of T cell proliferation. [GOC:jl] |