While Aspirin is typically used by patients prone to heart disease, there are many hypotheses about its other potential therapeutic benefits, such as a chemotherapy or a preventive of preeclampsia. Aspirin inhibits the COX enzymes by acetylating critical active site residues, leaving the enzymes acatalytic while generating salicylic acid (SA) as a byproduct. Aspirin is a known cyclooxygenase (COX) inhibitor, giving the molecule its anti-inflammatory and blood thinning characteristics. These carboxylic acid-based compounds represent a new and largely unstudied class of CAIs.Īspirin (acetylsalicylic acid) is one of the most widely studied and consumed drugs in use. Previous work has also shown that salicylic acid as well as some phenol derivatives are μM inhibitors of mammalian CAs, although the exact mechanism of inhibition for salicylic acid is unknown. Furthermore, 3-nitrobenzoic acid has also been reported as a potent CAI, with further studies showing its potential clinical relevance as a cancer therapeutic. Unlike the sulfonamide-based drugs, these inhibitors do not directly displace the zinc bound solvent, but instead anchor through the solvent, blocking substrate entry to the active site. Nicotinic and ferulic acid have recently been identified as inhibitors of CAII. In addition to sulfonamides, a variety of other chemical motifs have been identified to inhibit CA, such as carboxylic acids. Many of these sulfonamide-based molecules are used clinically, such as dorzolamide, for the treatment of glaucoma. The most common type of CAIs are sulfonamides, such as acetazolamide, which has nM binding affinity. These inhibitors are designed to bind to the active site zinc, displacing the zinc bound solvent. In addition, CAIs are currently being developed as anti-cancer drugs. CA inhibitors (CAIs) are used to treat a variety of diseases such as glaucoma, altitude sickness, and epilepsy. As CAs are responsible for a variety of physiological functions and pH regulation, they are often clinically targeted.
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