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Literature summary for 3.1.1.4 extracted from

  • Tai, N.; Kuwabara, K.; Kobayashi, M.; Yamada, K.; Ono, T.; Seno, K.; Gahara, Y.; Ishizaki, J.; Hori, Y.
    Cytosolic phospholipase A2 alpha inhibitor, pyrroxyphene, displays anti-arthritic and anti-bone destructive action in a murine arthritis model (2010), Inflamm. Res., 59, 53-62.
    View publication on PubMed

Application

Application Comment Organism
drug development potential therapeutic role for cPLA2 alpha inhibitors in the treatment of human rheumatoid arthritis. Oral administration of pyrroxyphene achieves anti-arthritic activity through inhibition of cPLA2 alpha activity, which leads to a reduction in eicosanoid levels and suppression of matrix metalloproteinases and cyclooxygenase-2 mRNA expression Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
pyrroxyphene significantly inhibits both the increase in levels of cPLA2 alpha and eicosanoids as well as the mRNA expression of matrix metalloproteinase-3, -8, -9, -13, and cyclooxygenase-2. Strongly inhibits the incidence of arthritis and bone destruction Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required for catalysis Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
male DBA/1J mice
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-palmitoyl-2-arachidonoylphosphatidylcholine + H2O
-
Mus musculus 1-palmitoyl-glycerophosphorylcholine + arachidonic acid
-
?

Synonyms

Synonyms Comment Organism
cPLA2 alpha
-
Mus musculus
cytosolic phospholipase A2 alpha
-
Mus musculus

General Information

General Information Comment Organism
physiological function cPLA2 alpha plays an important role in the pathogenesis of collagen-induced arthritis. cPLA2 alpha activity increases in hind paws of collagen-induced arthritic mice Mus musculus