| 货号 | 14944-250ug |
| 描述 | HMG-CoA reductase (HMGR) is a highly regulated enzyme found on the endoplasmic reticulum (ER) membrane. It is bound to the ER membrane by a multi-pass 339 amino acid N-terminal transmembrane domain while the carboxy terminal catalytic region projects into the cytosol.1,2 HMGR is controlled by feedback regulation from sterols and non-sterol metabolites derived from mevalonate.2,3,4 Binding of cholesterol derived from internalized LDL receptors suppresses HMGR. The enzyme is responsible for catalyzing the rate-limiting step in cholesterol biosynthesis. Mevalonate, which is converted to isopentenyl pyrophosphate, is the building block for cholesterol and non-sterol isoprenoids. The four-electron reduction of HMG-CoA catalyzed by HMGR to form mevalonate is the committed step in the biosynthesis of sterols and isoprenoids.5 Potent inhibitors of HMGR, collectively called statins, are effective in lowering mortality due to hypercholesterolemia by lowering serum cholesterol levels.6 |
| 别名 | 3-hydroxy-3-methylglutaryl-Coenzyme A Reductase;HMGCR;HMGR; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Istvan, E.S.,Palnitkar, M.,Buchanan, S.K., et al. Crystal structure of the catalytic portion of human HMG-CoA reductase: Insights into regulation of activity and catalysis. EMBO Journal 19(5), 819-830 (2000). 2.Luskey, K.L. and Stevens, B. Human 3-hydroxy-3-methylglutaryl coenzyme A reductase. Conserved domains responsible for catalytic activity and sterol-regulated degradation. The Journal of Biological Chemisty 260(18), 10271-10277 (1985). 3.Brown, M.S. and Goldstein, J.L. Multivalent feedback regulation of HMG CoA reductase, a control mechanism coordinating isoprenoid synthesis and cell growth. Journal of Lipid Research 21(5), 505-517 (1980). 4.Sever, N.,Yang, T.,Brown, M.S., et al. Accelerated degradation of HMG CoA reductase mediated by binding of insig-1 to its sterol-sensing domain. Mol.Cell. 11(1), 25-33 (2003). 5.Istvan, E.S. and Deisenhofer, J. Structural mechanism for statin inhibition of HMG-CoA reductase. Science 292, 1160-1164 (2001). 6.Brown, W.V. Safety of statins. Current Opinion in Lipidology 19(6), 558-562 (2008). | |
| 运输条件 | Dry ice in continental US; may vary elsewhere |
| 存放说明 | -80 |
| 纯度 | ≥90% estimated by SDS-PAGE |
| 稳定性 | ≥ 9 months |
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