| Autor: |
Zupan LA; Department of Internal Medicine, Washington University School of Medicine, St. Louis, Missouri 63110., Weiss RH, Hazen SL, Parnas BL, Aston KW, Lennon PJ, Getman DP, Gross RW |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1993 Jan 08; Vol. 36 (1), pp. 95-100. |
| DOI: |
10.1021/jm00053a012 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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