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. 2006 Jun;7(6):971-80.
doi: 10.1002/cbic.200500454.

The molecular mechanism of bee venom phospholipase A2 inactivation by bolinaquinone

Maria Chiara Monti  1 , Agostino Casapullo, Cosima Santomauro, Maria Valeria D'Auria, Raffaele Riccio, Luigi Gomez-Paloma
Affiliations

The molecular mechanism of bee venom phospholipase A2 inactivation by bolinaquinone

Maria Chiara Monti et al. Chembiochem. 2006 Jun.

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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