July 1, 1994Biochemistry
Rapid Inactivation of Prostaglandin Endoperoxide Synthases by N-(Carboxyalkyl)maleimides
Population
Ovine PGHS-1, and mouse and human PGHS-2 enzymes
Comparison
N-maleimides, specifically N-maleimide vs N--succinimide and aspirin
Design
Preclinical
Authors
Discussion
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Member takes
Implication
Potent PGHS inactivation in biochemical assays merits selectivity studies; leaves open in vivo efficacy and human translation.
Structured PICO
P
Population
Ovine PGHS-1, and mouse and human PGHS-2 enzymes
I
Intervention
N-(Carboxyalkyl)maleimides, specifically N-(carboxyheptyl)maleimide
C
Comparator
N-(Carboxyheptyl)-succinimide and aspirin (reference)
O
Outcome
Inhibition of cyclooxygenase and peroxidase activities (IC50)surrogate
N-(Carboxyheptyl)maleimide is a highly potent covalent inactivator of PGHS, with an inhibitory potency 3-5 orders of magnitude greater than aspirin.
Cite This Study
Kalgutkar et al. (1994) studied this question.