The molecular mechanism of bee venom phospholipase A2 inactivation by bolinaquinone |
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| Authors: | Monti Maria Chiara Casapullo Agostino Santomauro Cosima D'Auria Maria Valeria Riccio Raffaele Gomez-Paloma Luigi |
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| Affiliation: | Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno via Ponte don Melillo, 84084 Fisciano SA, Italy. |
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| Abstract: | The molecular basis of the inactivation of bee venom PLA2 by the marine natural product bolinaquinone (BLQ) was studied by several spectral techniques (CD, fluorescence, and NMR spectroscopy, mass spectrometry), biomimetic reactions, and molecular modeling. Our data suggest competitive inhibition based on a BLQ-PLA2 noncovalent molecular recognition. However, BLQ is also able to react selectively with Lys133 through conjugate addition followed by a beta elimination. The biological implications of both the covalent and noncovalent molecular events are discussed. |
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| Keywords: | enzyme inhibition marine natural products mechanistic studies molecular recognition phospholipases |
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