PLA 2 G 4 A ( phospholipase A 2 , group IVA ( cytosolic , calcium - dependent ) )
نویسندگان
چکیده
Description cPLA2alpha is an 85 kDa protein consisting of 749 amino acids. cPLA2alpha belongs to the alpha-beta hydrolase family which is identified by a characteristic nucleophile elbow with a consensus sequence of Sm-X-Nu-Sm (Sm = small residue, X = any residue and Nu = nucleophile). The protein contains an N-terminal C2 domain (Cadependent, phospholipid binding) and two catalytic domains (alpha/beta hydrolase). The N-terminal region of the first catalytic domain contains the lipase consensus sequence, GXSGS. At the active site, cPLA2alpha contains a serine nucleophile (Ser228) through which the catalytic mechanism is initiated.
منابع مشابه
Platelet-activating factor production in the spinal cord of experimental allergic encephalomyelitis mice via the group IVA cytosolic phospholipase A2-lyso-PAFAT axis.
Platelet-activating factor (PAF; 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine) plays a critical role in inflammatory disorders including experimental allergic encephalomyelitis (EAE), an animal model for multiple sclerosis (MS). Although PAF accumulation in the spinal cord (SC) of EAE mice and cerebrospinal fluid of MS patients has been reported, little is known about the metabolic processing...
متن کاملSystemic and intrathecal effects of a novel series of phospholipase A2 inhibitors on hyperalgesia and spinal prostaglandin E2 release.
Phospholipase A(2) (PLA(2)) forms are expressed in spinal cord, and inhibiting spinal PLA(2) induces a potent antihyperalgesia. Here, we examined the antihyperalgesic effects after systemic and i.t. delivery of four compounds constructed with a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four-carbon tether. These molecules were characterized for their ability to block ...
متن کاملNovel 2-oxoamide inhibitors of human group IVA phospholipase A(2).
A novel class of potent human cytosolic phospholipase A(2) (GIVA PLA(2)) inhibitors was developed. These inhibitors were designed to contain the 2-oxoamide functionality and a free carboxyl group. Among the compounds tested, a long-chain 2-oxoamide containing L-gamma-norleucine was the most potent inhibitor, causing a 50% decrease in GIVA PLA(2) activity at 0.009 mole fraction.
متن کاملIdentification of intracellular phospholipases A2 in the human eye: involvement in phagocytosis of photoreceptor outer segments.
PURPOSE To identify intracellular phospholipases A(2) (PLA(2)) in the human retina and to explore the role of these enzymes in human retinal pigment epithelium (RPE) phagocytosis of photoreceptor outer segments (POS). METHODS PCR amplification and Western blot analysis were used to identify mRNA and protein expression of intracellular PLA(2) subtypes in the retinal pigment epithelial cell lin...
متن کاملIntracellular phospholipase A(2) group IVA and group VIA play important roles in Wallerian degeneration and axon regeneration after peripheral nerve injury.
We provide evidence that two members of the intracellular phospholipase A(2) family, namely calcium-dependent group IVA (cPLA(2) GIVA) and calcium-independent group VIA (iPLA(2) GVIA) may play important roles in Wallerian degeneration in the mouse sciatic nerve. We assessed the roles of these PLA(2)s in cPLA(2) GIVA(-/-) mice, and mice treated with a selective inhibitor of iPLA(2) GVIA (FKGK11)...
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