Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors

  title={Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors},
  author={Jonathan A. Tobert},
  journal={Nature Reviews Drug Discovery},
  • J. Tobert
  • Published 1 July 2003
  • Biology
  • Nature Reviews Drug Discovery
In the 1950s and 1960s, it became apparent that elevated concentrations of plasma cholesterol were a major risk factor for the development of coronary heart disease, which led to the search for drugs that could reduce plasma cholesterol. One possibility was to reduce cholesterol biosynthesis, and the rate-limiting enzyme in the cholesterol biosynthetic pathway, 3-hydroxy-3-methyl-glutaryl-CoA (HMG-CoA) reductase, was a natural target. Here, I describe the discovery and development of lovastatin… 
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Inhibitors of the rate-limiting enzyme of cholesterol biosynthesis, 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase, are now used frequently to treat hypercholesterolemia and results in an increased expression of hepatic LDL receptors, which explains the lowered plasma levels of LDL cholesterol.
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