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- W2079624387 abstract "Subsequent to the discovery of compactin (ML-236B) as a specific inhibitor of HMG CoA reductase, a series of compactin analogs have been either isolated or synthesized. Several of these compounds, which include compactin, mevinolin (monacolin K) and CS-514, have been extensively studied. The inhibition of HMG CoA reductase by these compounds is reversible and competitive (Ki = ∼ 1 nM). The 3′, 5′-dihydroxypentanoic acid portion of the acid form of compactin analogs, which resembles the HMG portion of HMG CoA, plays a crucial role in inhibitory activity. These inhibitors block sterol synthesis both in cultured mammalian cells and in animals. Strong inhibition of sterol synthesis results in a marked increase in HMG CoA reductase activity both in vitro and in vivo. These compounds strongly lower plasma LDL-cholesterol levels in animals and humans. The lowering of LDL-cholesterol levels occurs by an inhibition of LDL synthesis and/or by an elevation of the receptor-mediated LDL catabolism in the liver." @default.
- W2079624387 created "2016-06-24" @default.
- W2079624387 creator A5006109788 @default.
- W2079624387 creator A5029659497 @default.
- W2079624387 date "1989-01-01" @default.
- W2079624387 modified "2023-10-04" @default.
- W2079624387 title "Biochemical aspect of HMG CoA reductase inhibitors" @default.
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- W2079624387 doi "https://doi.org/10.1016/0065-2571(89)90063-0" @default.
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