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An Alpha-Mercaptoacrylic Acid Derivative is a Selective Nonpeptide Cell-Permeable Calpain Inhibitor and is Neuroprotective
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An Alpha-Mercaptoacrylic Acid Derivative is a Selective Nonpeptide Cell-Permeable Calpain Inhibitor and is Neuroprotective
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Journal Article
An Alpha-Mercaptoacrylic Acid Derivative is a Selective Nonpeptide Cell-Permeable Calpain Inhibitor and is Neuroprotective
1996
Overview
Overactivation of calcium-activated neutral protease (calpain) has been implicated in the pathophysiology of several degenerative conditions, including stroke, myocardial ischemia, neuromuscular degeneration, and cataract formation. Alpha-mercaptoacrylate derivatives (exemplified by PD150606), with potent and selective inhibitory actions against calpain, have been identified. PD150606 exhibits the following characteristics: (i) Ki values for μ - and m-calpains of 0.21 μ M and 0.37 μ M, respectively, (ii) high specificity for calpains relative to other proteases, (iii) uncompetitive inhibition with respect to substrate, and (iv) it does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane, suggesting a nonactive site action for PD150606. The recombinant calcium-binding domain from each of the large or small subunits of μ -calpain was found to interact with PD150606. In low micromolar range, PD150606 inhibited calpain activity in two intact cell systems. The neuroprotective effects of this class of compound were also demonstrated by the ability of PD150606 to attenuate hypoxic/hypoglycemic injury to cerebrocortical neurons in culture and excitotoxic injury to Purkinje cells in cerebellar slices.
Publisher
National Academy of Sciences of the United States of America,National Acad Sciences,National Academy of Sciences
Subject
/ alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid - toxicity
/ Animals
/ Calcium
/ Cells
/ Cerebral Cortex - drug effects
/ Cysteine Proteinase Inhibitors - pharmacology
/ Enzymes
/ Gels
/ Glycoproteins - pharmacology
/ Hypoglycemia - physiopathology
/ Hypoxia
/ Kinetics
/ Neurons
/ Purkinje Cells - drug effects
/ Rats
