Date published: 2025-9-11

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GST Activators

GST activators are a class of chemical compounds that enhance the activity of Glutathione S-transferases (GSTs), a family of enzymes that play a crucial role in cellular detoxification and protection against oxidative stress. These enzymes are quite ubiquitous, found in virtually all organisms, from bacteria to humans. They catalyze the conjugation of the reduced form of glutathione (GSH), a tripeptide, to electrophilic centers on a wide variety of substrates. This process, known as glutathione conjugation, aids in the transformation of harmful compounds, such as reactive oxygen species and xenobiotics, into more soluble, and therefore more easily excretable, forms.GST activators function by binding to the GST enzyme, often at a site distinct from the active site, subsequently altering the enzyme's conformation. This alteration can increase the enzyme's affinity for its substrates, enhance the rate of catalysis, or both. The specifics of this interaction can vary depending on the activator in question and the particular GST enzyme it targets. GSTs are a large and diverse family of enzymes, grouped into several classes based on sequence similarityeach with unique substrate specificities and inhibitor sensitivities. As a result, GST activators can be just as diverse, with different activators optimized for interaction with different GST classes. Despite this diversity, the end result is the same: an increase in glutathione conjugation activity, assisting in the management of oxidative stress and detoxification processes at a cellular level. The study of GST activators thus contributes significantly to our understanding of cellular protection mechanisms and regulation of oxidative stress.

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