%0 Journal Article
%T PLA2-mediated catalytic activation of its inhibitor 25-acetyl-petrosaspongiolide M: serendipitous identification of a new PLA2 suicide inhibitor
%J FEBS letters
%D 2004
%A Monti, M. C.
%A Casapullo, A.
%A Riccio, R.
%A Gomez-Paloma, L.
%V 578
%N 3
%P 269-274
%X 25-Acetyl-petrosaspongiolide M (PMAc) (1), a mild non-covalent PLA(2) inhibitor, unexpectedly recovers, after incubation with bvPLA(2), the ability to covalently modify the enzyme target. This study demonstrates the catalytic effect of bvPLA(2) in converting 1 in its deacetylated congener petrosaspongiolide M (PM) (2), a strong covalent PLA(2) inhibitor whose molecular mechanism of inhibition has already been clarified. Moreover, our findings outline the potential role of PMAc as anti-inflammatory pro-drug, by virtue of its ability of delivering the active PM agent at the site of inflammation, functioning as a suicide inhibitor.<p /><p>Language: en</p>
%G en
%I Elsevier Publishing
%@ 0014-5793
%U http://dx.doi.org/10.1016/j.febslet.2004.10.100