What is it about?
This publication reveals the substrate specificity of the mevalonate pathway regulatory enzyme HMG-CoA reductase (EC 1.1.1.1.88). This allows a different perspective on the search and discovery of new drugs related to the treatment of elevated cholesterol levels in patients with various lipid metabolism disorders.
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Why is it important?
We consider enzyme action in terms of those substrates and inhibitors that can bind to the active center of the HMG-CoA reductase enzyme. The study and analysis of these mechanisms allows us to understand in detail how the regulatory enzyme of this metabolic pathway works and to take a new look at how the enzyme works. It is assumed that competitive inhibitors of this enzyme can also be substrates for it, but due to the lower reaction rate and inhibition of reactions of the metabolic pathway (metabolism of HMG-CoA and synthesis of terpenoid chain) associated with the active center of the inhibitor compound, which allows to reduce the level of cholesterol in the patient's blood.
Perspectives
Research in this area allows us to reconsider the mechanisms of enzyme activity and the approach to the development of new enzyme inhibitors, the study of substrates, products and intermediates of enzymatic reaction expands the range of potential inhibitor compounds, and gives new life to research directions for the development of clinically necessary inhibitor drugs
Ilya Kuzminov
Tyumen state medical university
Read the Original
This page is a summary of: New Aspects in the Mechanism of Action of 3-hydroxy-3-methylglutaryl- COA Reductase (HMG-CoA reductase): Cyclic Lactones - Potential Inhibitors of the Enzyme (Review), Current Enzyme Inhibition, October 2024, Bentham Science Publishers,
DOI: 10.2174/0115734080298814240528092106.
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