Fluvastatin: Difference between revisions
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===Mechanism of Action=== | ===Mechanism of Action=== | ||
Fluvastatin is an inhibitor of [[HMG-CoA Reductase]] (HMGR), a highly regulated enzyme responsible for the committed step in cholesterol synthesis. Fluvastatin outcompetes HMG-CoA, the substrate of HMGR, in binding to HMGR.<ref>PMID:7784310</ref> | Fluvastatin is an inhibitor of [[HMG-CoA Reductase]] (HMGR), a highly regulated enzyme responsible for the committed step in cholesterol synthesis. Fluvastatin outcompetes HMG-CoA, the substrate of HMGR, in binding to HMGR.<ref>PMID:7784310</ref> | ||
Fluvastatin, like most of the statins, <scene name='Fluvastatin/Statin_fluva/1'>binds HMGR</scene> via a number of polar interactions with the "cis loop" of HMGR, particularly residues Ser 684, Asp 690, Lys 691, Lys 692, and hydrogen bond interactions between Glu 559 and Asp 767 with the O5-hydroxyl of the statins. Van der Waals interactions between Leu 562, Val 683, Leu 853, Ala 856, and Leu 857 of HMGR and hydrophobic ring structures of Fluvastatin contribute to binding as well.<ref>PMID:11349148</ref> These interactions help Fluvastatin outcompete HMG-CoA, the substrate of HMGR, in binding to HMGR.<ref>PMID:7784310</ref> | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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