Date published: 2025-11-3

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mEH Activators

mEH activators are a category of chemical agents specifically designed to enhance the enzymatic activity of microsomal epoxide hydrolase (mEH), a critical detoxifying enzyme that catalyzes the conversion of epoxides to diols. This biotransformation is an essential part of the body's mechanism to process and eliminate potentially harmful xenobiotic and endogenous compounds, thereby mitigating their potential toxicity and mutagenic effects. mEH is thus a key player in the metabolism of a wide range of epoxide substrates that result from the oxidation of various lipids, drugs, and environmental contaminants.

Activators of mEH can function through direct or indirect means. Direct activators may bind to the active site or to allosteric sites on the enzyme, leading to a conformational change that increases the enzyme's catalytic efficiency. By enhancing the affinity of mEH for its substrates or by stabilizing the transition state of the reaction, these activators can increase the rate of hydrolysis of epoxides to less reactive diols. This can result in a more efficient processing of substrates through the enzyme's active site and an increased turnover rate. Indirect activators, on the other hand, may affect mEH activity by modulating the expression of the enzyme or by influencing post-translational modifications that alter enzyme function. Cellular signaling pathways, transcription factors, and epigenetic modifications may all play a role in regulating the levels of mEH within the cell, and compounds that affect these pathways can lead to increased enzyme expression and activity. Additionally, post-translational modifications such as phosphorylation or glycosylation could affect the stability, localization, or interaction of mEH with other cellular components, thereby indirectly influencing its activity.

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