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A historical perspective on the discovery of statins.

Endo A - Proc. Jpn. Acad., Ser. B, Phys. Biol. Sci. (2010)

Bottom Line: Cholesterol is essential for the functioning of all human organs, but it is nevertheless the cause of coronary heart disease.Over the course of nearly a century of investigation, scientists have developed several lines of evidence that establish the causal connection between blood cholesterol, atherosclerosis, and coronary heart disease.Building on that knowledge, scientists and the pharmaceutical industry have successfully developed a remarkably effective class of drugs--the statins--that lower cholesterol levels in blood and reduce the frequency of heart attacks.

View Article: PubMed Central - PubMed

Affiliation: Biopharm Research Laboratories, Inc., Tokyo 181-0013, Japan. aendo@biopharm.co.jp

ABSTRACT
Cholesterol is essential for the functioning of all human organs, but it is nevertheless the cause of coronary heart disease. Over the course of nearly a century of investigation, scientists have developed several lines of evidence that establish the causal connection between blood cholesterol, atherosclerosis, and coronary heart disease. Building on that knowledge, scientists and the pharmaceutical industry have successfully developed a remarkably effective class of drugs--the statins--that lower cholesterol levels in blood and reduce the frequency of heart attacks.

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Related in: MedlinePlus

Structual similarities between compactin and HMG-CoA.
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Related In: Results  -  Collection


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fig02: Structual similarities between compactin and HMG-CoA.

Mentions: HMG-CoA reductase is the rate-controlling enzyme in cholesterol synthesis. We soon realized the structural similarities between compactin and HMG-CoA, the substrate of the HMG-CoA reductase reaction55,57) (Fig. 2). The structure of compactin was exactly as we had previously envisioned. Compactin was an extremely potent inhibitor of HMG-CoA reductase, and its mechanism of action, as suggested by its structure, was that of a competitive inhibitor.57) I had set my sights on finding a competitive inhibitor of HMG-CoA reductase, and compactin seemed to be a wonderful gift from nature.


A historical perspective on the discovery of statins.

Endo A - Proc. Jpn. Acad., Ser. B, Phys. Biol. Sci. (2010)

Structual similarities between compactin and HMG-CoA.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3108295&req=5

fig02: Structual similarities between compactin and HMG-CoA.
Mentions: HMG-CoA reductase is the rate-controlling enzyme in cholesterol synthesis. We soon realized the structural similarities between compactin and HMG-CoA, the substrate of the HMG-CoA reductase reaction55,57) (Fig. 2). The structure of compactin was exactly as we had previously envisioned. Compactin was an extremely potent inhibitor of HMG-CoA reductase, and its mechanism of action, as suggested by its structure, was that of a competitive inhibitor.57) I had set my sights on finding a competitive inhibitor of HMG-CoA reductase, and compactin seemed to be a wonderful gift from nature.

Bottom Line: Cholesterol is essential for the functioning of all human organs, but it is nevertheless the cause of coronary heart disease.Over the course of nearly a century of investigation, scientists have developed several lines of evidence that establish the causal connection between blood cholesterol, atherosclerosis, and coronary heart disease.Building on that knowledge, scientists and the pharmaceutical industry have successfully developed a remarkably effective class of drugs--the statins--that lower cholesterol levels in blood and reduce the frequency of heart attacks.

View Article: PubMed Central - PubMed

Affiliation: Biopharm Research Laboratories, Inc., Tokyo 181-0013, Japan. aendo@biopharm.co.jp

ABSTRACT
Cholesterol is essential for the functioning of all human organs, but it is nevertheless the cause of coronary heart disease. Over the course of nearly a century of investigation, scientists have developed several lines of evidence that establish the causal connection between blood cholesterol, atherosclerosis, and coronary heart disease. Building on that knowledge, scientists and the pharmaceutical industry have successfully developed a remarkably effective class of drugs--the statins--that lower cholesterol levels in blood and reduce the frequency of heart attacks.

Show MeSH
Related in: MedlinePlus