Literature summary 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.
Application
EC Number |
Application |
Comment |
Organism |
---|
3.1.1.4 |
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
EC Number |
Inhibitors |
Comment |
Organism |
Structure |
---|
3.1.1.4 |
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
EC Number |
Localization |
Comment |
Organism |
GeneOntology No. |
Textmining |
---|
Metals/Ions
EC Number |
Metals/Ions |
Comment |
Organism |
Structure |
---|
3.1.1.4 |
Ca2+ |
required for catalysis |
Mus musculus |
|
Organism
EC Number |
Organism |
UniProt |
Comment |
Textmining |
---|
3.1.1.4 |
Mus musculus |
- |
male DBA/1J mice |
- |
Substrates and Products (Substrate)
EC Number |
Substrates |
Comment Substrates |
Organism |
Products |
Comment (Products) |
Rev. |
Reac. |
---|
3.1.1.4 |
1-palmitoyl-2-arachidonoylphosphatidylcholine + H2O |
- |
Mus musculus |
1-palmitoyl-glycerophosphorylcholine + arachidonic acid |
- |
? |
|
Synonyms
EC Number |
Synonyms |
Comment |
Organism |
---|
3.1.1.4 |
cPLA2 alpha |
- |
Mus musculus |
3.1.1.4 |
cytosolic phospholipase A2 alpha |
- |
Mus musculus |
General Information
EC Number |
General Information |
Comment |
Organism |
---|
3.1.1.4 |
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 |