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PDBsum entry 3o4m
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Hydrolase/hydrolase inhibitor
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PDB id
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3o4m
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References listed in PDB file
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Key reference
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Title
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Binding to pla2 may contribute to the anti-Inflammatory activity of catechol.
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Authors
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K.V.Dileep,
I.Tintu,
P.K.Mandal,
P.Karthe,
M.Haridas,
C.Sadasivan.
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Ref.
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Chem Biol Drug Des, 2012,
79,
143-147.
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PubMed id
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Note: In the PDB file this reference is
annotated as "TO BE PUBLISHED". The citation details given above have
been manually determined.
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Abstract
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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.
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