| Literature DB >> 8421294 |
L A Zupan1, R H Weiss, S L Hazen, B L Parnas, K W Aston, P J Lennon, D P Getman, R W Gross.
Abstract
Haloenol lactones are potent mechanism-based inhibitors of a novel class of calcium-independent phospholipases A2 which have been implicated as the enzymic mediators of membrane dysfunction during myocardial ischemia (Hazen, S. L.; et al. J. Biol. Chem. 1991, 266, 7227-7232). Herein we demonstrate that the ring size, hydrophobic group, and cryptic electrophile in the haloenol lactone moiety are important and modifiable determinants of the inhibitory potency of haloenol lactone-mediated inhibition of calcium-independent phospholipase A2. Direct comparisons between haloenol lactone-mediated inhibition of calcium-independent phospholipase A2 and the absence of inhibition with calcium-dependent phospholipase A2 further underscore the marked differences in the catalytic strategy employed by these two classes of intracellular phospholipases A2.Entities:
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Year: 1993 PMID： 8421294 DOI： 10.1021/jm00053a012
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446