Journal ArticleDOI
Competitive inhibition of 3-hydroxy-3-methylglutaryl coenzyme a reductase by ML-236A and ML-236B fungal metabolites, having hypocholesterolemic activity
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TLDR
The experiments reported in this paper demonstrate that MG236A and ML-236B inhibit specifically 3-hydroxy-3-methylglutaryl (HMG)CoA reductase (EC 1 .I .1.34), the rate-limiting enzyme in cholesterol synthetic pathway, without affecting the rest of the enzymes involved in this pathway, and that the inhibition is competitive with respect to the substrate HMG-CoA.About:
This article is published in FEBS Letters.The article was published on 1976-12-31. It has received 699 citations till now. The article focuses on the topics: Hydroxymethylglutaryl-CoA reductase & Non-competitive inhibition.read more
Citations
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A receptor-mediated pathway for cholesterol homeostasis.
TL;DR: The approach was to apply the techniques of cell culture to unravel the postulated regulatory defect in FH, which led to the discovery of a cell surface receptor for a plasma cholesterol transport protein called low density lipoprotein (LDL) and to the elucidation of the mechanism by which this receptor mediates feedback control of cholesterol synthesis.
Journal ArticleDOI
Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent.
Alfred W. Alberts,Julie S. Chen,G Kuron,V Hunt,Jesse W. Huff,Carl H. Hoffman,John W. Rothrock,Lopez Maria B,Henry Joshua,Elbert E. Harris,Arthur A. Patchett,R L Monaghan,S Currie,E Stapley,George Albers-Schonberg,Otto D. Hensens,J Hirshfield,Karst Hoogsteen,Jerrold M. Liesch,James P. Springer +19 more
TL;DR: It was shown that mevinolin was an orally active cholesterol-lowering agent in the dog and orally administered sodium mevinolinate was an active inhibitor of cholesterol synthesis in an acute assay.
Journal ArticleDOI
Structural mechanism for statin inhibition of HMG-CoA reductase.
Eva S. Istvan,Johann Deisenhofer +1 more
TL;DR: The structures of the catalytic portion of human HMGR complexed with six different statins are determined, which show several catalytically relevant residues are disordered in the enzyme-statin complexes.
Journal ArticleDOI
Nitrogen-Containing Bisphosphonates Inhibit the Mevalonate Pathway and Prevent Post-Translational Prenylation of GTP-Binding Proteins, Including Ras
Steven P. Luckman,Steven P. Luckman,D. E. Hughes,F P Coxon,F P Coxon,R. Graham G. Russell,Michael J. Rogers +6 more
TL;DR: Nitrogen‐containing bisphosphonate drugs cause apoptosis following inhibition of post‐translational prenylation of proteins such as Ras, and the data support the view that clodronate acts by a different mechanism.
Journal ArticleDOI
Multivalent feedback regulation of HMG CoA reductase, a control mechanism coordinating isoprenoid synthesis and cell growth
TL;DR: The availability of compactin (ML-236B), a potent competitive inhibitor of 3-hydroxy-3-methylglutaryl Coenzyme A reductase, has permitted the demonstration of a hitherto unsuspected aspect of mevalonate metabolism and isoprenoid synthesis in cultured mammalian cells.
References
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Journal Article
Protein Measurement with the Folin Phenol Reagent
TL;DR: Procedures are described for measuring protein in solution or after precipitation with acids or other agents, and for the determination of as little as 0.2 gamma of protein.
Journal ArticleDOI
Inhibition of in vitro cholesterol synthesis by fatty acids.
Kuroda Masao,Endo Akira +1 more
TL;DR: The highly unsaturated fatty acids, arachidonate and linoleate, were specific inhibitors of 3-hydroxy-3-methyl-glutaryl-CoA synthase and ricinoleate and phytanate diminished the conversion of mevalonate to sterols by inhibiting a step or steps between squalene and lanosterol.
Journal ArticleDOI
Solubilization and partial purification of hepatic 3-hydroxy-3-methylglutaryl coenzyme A reductase.
Renu A. Heller,R. Gordon Gould +1 more
TL;DR: An effective method for the solubilization of microsomal HMG-CoA reductase from rat liver by exposing the microsomes to a freeze-thaw treatment and a 25-fold purification led to an enzyme preparation with a specific activity and an increased stability.
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Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent.
Alfred W. Alberts,Julie S. Chen,G Kuron,V Hunt,Jesse W. Huff,Carl H. Hoffman,John W. Rothrock,Lopez Maria B,Henry Joshua,Elbert E. Harris,Arthur A. Patchett,R L Monaghan,S Currie,E Stapley,George Albers-Schonberg,Otto D. Hensens,J Hirshfield,Karst Hoogsteen,Jerrold M. Liesch,James P. Springer +19 more