TY  - JOUR
PY  - 1993//
TI  - Structural determinants of haloenol lactone-mediated suicide inhibition of canine myocardial calcium-independent phospholipase A2
JO  - Journal of medicinal chemistry
A1  - Zupan, L. A.
A1  - Weiss, R. H.
A1  - Hazen, S. L.
A1  - Parnas, B. L.
A1  - Aston, K. W.
A1  - Lennon, P. J.
A1  - Getman, D. P.
A1  - Gross, R. W.
SP  - 95
EP  - 100
VL  - 36
IS  - 1
N2  - 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.<p /> <p>Language: en</p>
LA  - en
SN  - 0022-2623
UR  - http://dx.doi.org/10.1021/jm00053a012
ID  - ref1
ER  -