Structural highlights
3o4m is a 1 chain structure with sequence from Sus scrofa. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , |
| Related: | 3hsw, 3l30, 3l69, 2b00, 2b03, 2b04 |
| Activity: | Phospholipase A(2), with EC number 3.1.1.4 |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
[PA21B_PIG] PA2 catalyzes the calcium-dependent hydrolysis of the 2-acyl groups in 3-sn-phosphoglycerides.
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
Inhibiting PLA(2) activity should, in theory, be an effective approach to control the inflammation. Several naturally occurring polyphenolic compounds have been reported as inhibitors of PLA(2) . Among the naturally occurring polyphenols, catechol (1,2-dihydroxybenzene) possesses anti-inflammatory activity. Catechol can inhibit cyclooxygenase and lipo-oxygenase. By means of enzyme kinetic study, it was revealed that catechol can inhibit PLA(2) also. Crystal structure showed that catechol binds to PLA(2) at the opening of the active site cleft. This might stop the entry of substrate into the active site. Hence, catechol can be used as a lead compound for the development of novel anti-inflammatory drugs with PLA(2) as the target.
Binding to PLA(2) May Contribute to the Anti-Inflammatory Activity of Catechol.,Dileep KV, Tintu I, Mandal PK, Karthe P, Haridas M, Sadasivan C Chem Biol Drug Des. 2011 Oct 13. doi: 10.1111/j.1747-0285.2011.01258.x. PMID:21995306[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Dileep KV, Tintu I, Mandal PK, Karthe P, Haridas M, Sadasivan C. Binding to PLA(2) May Contribute to the Anti-Inflammatory Activity of Catechol. Chem Biol Drug Des. 2011 Oct 13. doi: 10.1111/j.1747-0285.2011.01258.x. PMID:21995306 doi:10.1111/j.1747-0285.2011.01258.x
