@article{ref1,
title="PLA2-mediated catalytic activation of its inhibitor 25-acetyl-petrosaspongiolide M: serendipitous identification of a new PLA2 suicide inhibitor",
journal="FEBS letters",
year="2004",
author="Monti, M. C. and Casapullo, A. and Riccio, R. and Gomez-Paloma, L.",
volume="578",
number="3",
pages="269-274",
abstract="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>",
language="en",
issn="0014-5793",
doi="10.1016/j.febslet.2004.10.100",
url="http://dx.doi.org/10.1016/j.febslet.2004.10.100"
}