PLA2G2A: A Potential Drug Target for Inflammation and Pain (G5320)

Target Name: PLA2G2A

NCBI ID: G5320

PLA2G2A

PLA2G2A: A Potential Drug Target for Inflammation and Pain

PLA2G2A, a member of the group IIA phospholipase A2 (PLA2) family, is a protein that plays a crucial role in cellular signaling and inflammation. Discovered in 1995, PLA2G2A has been extensively studied for its role in various physiological processes, including inflammation, pain, and cellular signaling. As a result of these studies, PLA2G2A has gained significant interest as a potential drug target or biomarker.

The PLA2G2A gene, located on chromosome 14, encodes a 21-kDa protein that is expressed in various cell types. The protein has a catalytic active site, a calcium-dependent phosphorylating site, and a C-type tryptophanylalanine modification, which is known to play a structural and functional role in the protein.

Expression and function of PLA2G2A

PLA2G2A is a member of the PLA2 family, which includes three isoforms: PLA2, PLA2-associated protein (PAP), and PLA2-like. These isoforms differ in their N-terminus, which encodes a 24 amino acid residue. PLA2G2A, like the other isoforms in the PLA2 family, contains a catalytic active site, a calcium-dependent phosphorylating site, and a C-type tryptophanylalanine modification.

The PLA2G2A protein has been shown to play a crucial role in various cellular signaling pathways, including inflammation and pain signaling. For example, PLA2G2A has been shown to regulate the production of pro-inflammatory cytokines, such as TNF-伪 and IL-1尾, and to modulate the expression of anti-inflammatory cytokines, such as IL-10. PLA2G2A has also been shown to play a role in the regulation of cellular migration and the assembly of immune cells.

In addition to its role in cellular signaling, PLA2G2A has also been shown to be involved in the regulation of inflammation and pain signaling. For example, PLA2G2A has been shown to promote the production of pro-inflammatory cytokines and to contribute to the development of pain-induced muscle spasms.

Despite the extensive studies on PLA2G2A, the precise mechanism of its function remains poorly understood. Several studies have suggested that PLA2G2A may function as a negative regulator of the activity of various enzymes involved in cellular signaling, including the nuclear factor kappa B (NFKB) and the mitochondrial outer membrane protein (MOMP). These studies have also suggested that PLA2G2A may play a role in the regulation of cellular apoptosis.

As a potential drug target or biomarker, PLA2G2A has been the subject of intense research for its potential utility in the treatment of various diseases. Several studies have suggested that inhibition of PLA2G2A activity may be a promising strategy for the treatment of inflammatory and pain-related diseases. For example, several studies have shown that inhibition of PLA2G2A activity can effectively reduce the production of pro-inflammatory cytokines and improve pain relief in experimental models of inflammation and pain (10,11).

In conclusion, PLA2G2A is a protein that has been extensively studied for its role in various cellular signaling pathways, including inflammation and pain signaling. Its function as a negative regulator of cellular signaling and its potential as a drug target or biomarker make PLA2G2A an attractive target for the development of new therapies for

Protein Name: Phospholipase A2 Group IIA

Functions: Secretory calcium-dependent phospholipase A2 that primarily targets extracellular phospholipids with implications in host antimicrobial defense, inflammatory response and tissue regeneration (PubMed:10455175, PubMed:10681567, PubMed:2925633). Hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids (phospholipase A2 activity) with preference for phosphatidylethanolamines and phosphatidylglycerols over phosphatidylcholines (PubMed:10455175, PubMed:10681567). Contributes to lipid remodeling of cellular membranes and generation of lipid mediators involved in pathogen clearance. Displays bactericidal activity against Gram-positive bacteria by directly hydrolyzing phospholipids of the bacterial membrane (PubMed:11694541, PubMed:10358193). Upon sterile inflammation, targets membrane phospholipids of extracellular mitochondria released from activated platelets, generating free unsaturated fatty acids such as arachidonate that is used by neighboring leukocytes to synthesize inflammatory eicosanoids such as leukotrienes. Simultaneously, by compromising mitochondrial membrane integrity, promotes the release in circulation of potent damage-associated molecular pattern molecules that activate the innate immune response (PubMed:25082876). Plays a stem cell regulator role in the intestinal crypt. Within intracellular compartment mediates Paneth cell differentiation and its stem cell supporting functions by inhibiting Wnt signaling pathway in intestinal stem cell (ICS). Secreted in the intestinal lumen upon inflammation, acts in an autocrine way and promotes prostaglandin E2 synthesis that stimulates Wnt signaling pathway in ICS cells and tissue regeneration (By similarity). May play a role in the biosynthesis of N-acyl ethanolamines that regulate energy metabolism and inflammation. Hydrolyzes N-acyl phosphatidylethanolamines to N-acyl lysophosphatidylethanolamines, which are further cleaved by a lysophospholipase D to release N-acyl ethanolamines (PubMed:14998370). Independent of its catalytic activity, acts as a ligand for integrins (PubMed:18635536, PubMed:25398877). Binds to and activates integrins ITGAV:ITGB3, ITGA4:ITGB1 and ITGA5:ITGB1 (PubMed:18635536, PubMed:25398877). Binds to a site (site 2) which is distinct from the classical ligand-binding site (site 1) and induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:25398877). Induces cell proliferation in an integrin-dependent manner (PubMed:18635536)

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•   general information;
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•   expression level;
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•   advantages and risks of development, etc.
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