Gene Targets > calcium-dependent phospholipase A2 activity
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calcium-dependent phospholipase A2 activity

Definition

Target type: molecularfunction

Catalysis of the reaction: phosphatidylcholine + H2O = 1-acylglycerophosphocholine + a carboxylate. This reaction requires Ca2+. [EC:3.1.1.4]

Calcium-dependent phospholipase A2 (PLA2) activity is a crucial enzyme function involved in the hydrolysis of phospholipid molecules, specifically at the sn-2 position, releasing free fatty acids and lysophospholipids. This activity is tightly regulated by calcium ions, which bind to the enzyme and induce a conformational change, activating its catalytic site. The enzyme utilizes a water molecule to cleave the ester bond between the sn-2 fatty acid and the glycerol backbone of the phospholipid. PLA2 enzymes are diverse, with various isoforms exhibiting different substrate specificities, tissue distributions, and regulatory mechanisms. Their activity is vital in a range of cellular processes, including signaling pathways, inflammation, lipid metabolism, and membrane remodeling. In signal transduction, PLA2 activity generates arachidonic acid, a precursor for the biosynthesis of eicosanoids, including prostaglandins, thromboxanes, and leukotrienes, which are potent signaling molecules involved in inflammation, pain, and blood clotting. PLA2 also plays a role in membrane remodeling by hydrolyzing phospholipids, contributing to the reshaping of cell membranes and the release of bioactive lipids. Furthermore, PLA2 activity is implicated in various diseases, including cardiovascular disease, cancer, and neurological disorders. Its role in inflammation, immune response, and cell survival makes it a potential target for therapeutic intervention.'
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Proteins (14)

ProteinDefinitionTaxonomy
Cytosolic phospholipase A2 A cytosolic phospholipase A2 that is encoded in the genome of cow. [OMA:A4IFJ5, PRO:DNx]Bos taurus (cattle)
Cytosolic phospholipase A2 gammaA cytosolic phospholipase A2 gamma that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UP65]Homo sapiens (human)
Phospholipase A2 group VA phospholipase A2 group V that is encoded in the genome of human. [PRO:DNx, UniProtKB:P39877]Homo sapiens (human)
Putative inactive group IIC secretory phospholipase A2A group IIC secretory phospholipase A2 that is encoded in the genome of human. A substitution at a conserved active site residue likely renders it inactive. [PRO:DAN, UniProtKB:Q5R387]Homo sapiens (human)
Group IID secretory phospholipase A2A group IID secretory phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UNK4]Homo sapiens (human)
Group IIE secretory phospholipase A2A group IIE secretory phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NZK7]Homo sapiens (human)
Group 3 secretory phospholipase A2A group 3 secretory phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NZ20]Homo sapiens (human)
Group IIF secretory phospholipase A2A group IIF secretory phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9BZM2]Homo sapiens (human)
Group XIIA secretory phospholipase A2A group XIIA secretory phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9BZM1]Homo sapiens (human)
Cytosolic phospholipase A2A cytosolic phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P47712]Homo sapiens (human)
Phospholipase A2, membrane associatedA phospholipase A2, membrane associated that is encoded in the genome of human. [PRO:DNx, UniProtKB:P14555]Homo sapiens (human)
Cytosolic phospholipase A2 betaA cytosolic phospholipase A2 beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P0C869]Homo sapiens (human)
Phospholipase A2A phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P04054]Homo sapiens (human)
Group 10 secretory phospholipase A2A group 10 secretory phospholipase A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O15496]Homo sapiens (human)

Compounds (31)

CompoundDefinitionClassesRoles
quinacrinequinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9.

Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.		acridines;
aromatic ether;
organochlorine compound;
tertiary amino compound		antimalarial;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
indomethacinindometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.

Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.		aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic;
xenobiotic metabolite
nifedipineNifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
ici 204,219zafirlukast: a leukotriene D4 receptor antagonistcarbamate ester;
indoles;
N-sulfonylcarboxamide		anti-asthmatic agent;
leukotriene antagonist
4-bromophenacyl bromide4-bromophenacyl bromide: phospholipidase A(2) inhibitor; structure
oleanolic acidhydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite
ubenimexubenimex: growth inhibitor
5-benzyloxytryptophan
fpl 67047xxFPL 67047XX: inhibits phospholipase A2; structure in first source
3-octylthio-1,1,1-trifluoro-2-propanone3-octylthio-1,1,1-trifluoro-2-propanone: a pesticide synergist; inhibits juvenile hormone esterase
varespladibaromatic ether;
benzenes;
dicarboxylic acid monoamide;
indoles;
monocarboxylic acid;
primary carboxamide		anti-inflammatory drug;
antidote;
EC 3.1.1.4 (phospholipase A2) inhibitor
ly 311727LY 311727: a potent & selective inhibitor of human non-pancreatic secretory phospholipase A2; structure given in first source
cholic acidcholic acid : A bile acid that is 5beta-cholan-24-oic acid bearing three alpha-hydroxy substituents at position 3, 7 and 12.

Cholic Acid: A major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.		12alpha-hydroxy steroid;
3alpha-hydroxy steroid;
7alpha-hydroxy steroid;
bile acid;
C24-steroid;
trihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
arachidonic acidarachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.

icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.		icosa-5,8,11,14-tetraenoic acid;
long-chain fatty acid;
omega-6 fatty acid		Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite;
mouse metabolite
curcumincurcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.

Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.		aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
quercetin7-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
arachidonyltrifluoromethaneAACOCF3 : A fatty acid derivative that is arachidonic acid in which the OH part of the carboxy group has been replaced by a trifluoromethyl group

arachidonyltrifluoromethane: structure given in first source; inhibits 85-kDa phospholipase A2		fatty acid derivative;
ketone;
olefinic compound;
organofluorine compound		EC 3.1.1.4 (phospholipase A2) inhibitor
amentoflavonebiflavonoid;
hydroxyflavone;
ring assembly		angiogenesis inhibitor;
antiviral agent;
cathepsin B inhibitor;
P450 inhibitor;
plant metabolite
4-amylcinnamoylanthranilic acid4-amylcinnamoylanthranilic acid: phospholipase A2 inhibitor

N-(p-amylcinnamoyl)anthranilic acid : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 4-pentylcinnamoyl group. It is a transient receptor potential (TRP) channel blocker and phospholipase A2 (PLA2) inhibitor.		amidobenzoic acid;
cinnamamides;
secondary carboxamide		EC 3.1.1.4 (phospholipase A2) inhibitor;
TRP channel blocker
3-(4-octadecyl)benzoylacrylic acid
ochnaflavoneochnaflavone : A biflavonoid with an ether linkage between the B-rings of the apigenin and luteolin subunits. It has been isolated from several members of the Ochnaceae plant family.

ochnaflavone: from Lonicera japonica; structure given in first source		aromatic ether;
biflavonoid;
hydroxyflavone		anti-inflammatory agent;
antiatherogenic agent;
antibacterial agent;
EC 3.1.1.4 (phospholipase A2) inhibitor;
leukotriene antagonist;
plant metabolite
manoalidemanoalide : A sesterterpenoid isolated from the marine sponge Luffariella variabilis and which has been shown to exhibit inhibitory activity towards phospholipase A2.

manoalide: phospholipase A2 inhibitor; sesterterpene from marine sponge L. variabilis; structure given in first source		butenolide;
lactol;
sesterterpenoid		EC 3.1.1.4 (phospholipase A2) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
metabolite
manoaloguemanoalogue: synthetic analog of manoalide; phospholipase A2 antagonist; structure given in first source
ursodoxicoltaurinetauroursodeoxycholate : An organosulfonate oxoanion that is the conjugate base of tauroursodeoxycholic acid arising from deprotonation of the sulfonate OH group; major species at pH 7.3.

tauroursodeoxycholic acid : A bile acid taurine conjugate derived from ursoodeoxycholic acid.		bile acid taurine conjugateanti-inflammatory agent;
apoptosis inhibitor;
bone density conservation agent;
cardioprotective agent;
human metabolite;
neuroprotective agent
ym 26734YM 26734: inhibits group II phospholipase A2; structure given in first source
efipladibefipladib: structure in first source
indoxamindoxam: structure in first source
bolinaquinonebolinaquinone: a marine sesquiterpenoid from sponge Dysidea sp. with anti-inflammatory activity; structure in first source
cacospongionolide bcacospongionolide B: isolated from the sponge Fasciospongia cavernosa; structure in first source
methyl arachidonylfluorophosphonatephosphonic ester
pyrrophenonepyrrophenone: structure in first source
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