The molecular mechanism of bee venom phospholipase A2 inactivation by bolinaquinone

被引：20
作者：
Monti, Maria Chiara
Casapullo, Agostino
Santomauro, Cosima
D'Auria, Maria Valeria
Riccio, Raffaele
Gomez-Paloma, Luigi
机构：
[1] Univ Salerno, Dipartimento Sci Farmaceut, I-84084 Fisciano, SA, Italy
[2] Univ Naples Federico II, Dipartimento Chim Sostanze Nat, I-80131 Naples, Italy
来源：
CHEMBIOCHEM | 2006年 / 7卷 / 06期
关键词：
enzyme inhibition; marine natural products; mechanistic studies; molecular recognition; phospholipases;
D O I：
10.1002/cbic.200500454
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The molecular basis of the inactivation of bee venom PLA(2) 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-PLA(2) noncovalent molecular recognition. However, BLQ is also able to react selectively with Lys133 through conjugate addition followed by a P elimination. The biological implications of both the covalent and noncovalent molecular events are discussed.
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收藏
页码：971 / 980
页数：10
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