The molecular mechanism of bee venom phospholipase A2 inactivation by bolinaquinone.
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.
Monti
Maria Chiara
MC
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno via Ponte don Melillo, 84084 Fisciano SA, Italy.
Casapullo
Agostino
A
Santomauro
Cosima
C
D'Auria
Maria Valeria
MV
Riccio
Raffaele
R
Gomez-Paloma
Luigi
L