Mevastatin

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

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

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[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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