Mevastatin

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Mevastatin
Mevastatin.png
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
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Chemical and physical data
FormulaC23H36O6
Molar mass408.534 g/mol

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]


Overview

Mevastatin, compactin, ML-236B is a hypolipidemic agent that belongs to the statins class.

It was the first compound isolated in the 1970s during research into HMG-CoA reductase inhibitors produced by a mould Penicillium citrinum.

Nowadays, Mevastatin is not used in therapy of hyperlipidemias because of multiple side effects but it is the only source for production of other statin - pravastatin.

Mechanisms of Action

Mevastatin inhibits isoprenoid biosynthesis by inhibition of HMG-CoA reductase (Ki for acid form is 1 nM)1 and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans.[1] It causes cells to arrest early in the G1 phase. [2] [3]

Mevastatin is a close structural analog of lovastatin and both agents have the same biochemical and pharmacological activities. Mevastatin is inactive in cell-free assays. In cells however, it is hydrolyzed to the active free acid form by intracellular esterases.

References

  1. A. Endo J. Lipid Res. 1992 33 1569
  2. V. Quesney-Huneeus et al. J. Biol. Chem. 1983 258 378
  3. V. Quesney-Huneeus et al. Proc. Natl. Acad. Sci. USA 1979 76 5056

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