Molecular Enzymology and Drug Targets

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Enzymes and Drug Targets: Transition State Enzyme Inhibitors

Viyanka Amoria*

Enzyme inhibitors or inactivators are a common class of drugs used to treat cancer, inflammatory, cardiovascular, metabolic, and infectious diseases. Models exist for every one of the six classes of catalysts, however inhibitors of hydrolases, transferases, and oxidoreductases prevail. At concentrations of 100 nanomolars or less, enzyme inhibitors or inactivators that eventually become drugs typically have a high selectivity for their targets and a high potency toward their targets. Thirteen ribozymes make up the human CYP4 family of enzymes, which typically catalyse the -oxidation of endogenous fatty acids and eicosanoids. 20-HETE, a crucial signalling eicosanoid involved in regulating vascular tone and kidney reabsorption, can be biosynthesized by several CYP4 enzymes. Additionally, the rare genetic disorders Refsum disease and X-ALD are characterized by the accumulation of particular fatty acids. As a result, a potential approach for drug discovery is the inhibition or induction of CYP4 enzyme activity. The targeting of CYP4 enzymes in the development of new treatments for hypertension, stroke, certain cancers, and the fatty acid-linked orphan diseases is the subject of this review, which also includes a discussion of the substrate specificities, sites of expression, genetic regulation, and inhibition by exogenous chemicals of the human CYP4 enzymes. Either through a covalent reaction with nucleophilic enzyme residues or through noncovalent binding, drugs inhibits enzyme activity. The time-dependent loss of enzyme activity caused by affinity agents and mechanism-based inactivators' covalent inactivation is typically irreversible.


Hypertension; Stroke; Cancer; Refsum Disease; X-ALD

Published Date: 2022-12-30; Received Date: 2022-12-01