2q6c | pdb_00002q6c

Design and synthesis of novel, conformationally restricted HMG-COA reductase inhibitors

spinqualitylabelsall models 2q6c, resolution 2.00Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2q6c is a 4 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: HR1, SO4 Related: 2q1l, 2q6b Gene: HMGCR (HUMAN) Activity: Hydroxymethylglutaryl-CoA reductase (NADPH), with EC number 1.1.1.34 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [HMDH_HUMAN] Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins. Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models and may be useful for the treatment of hypercholesterolemia and related lipid disorders. Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors.,Pfefferkorn JA, Choi C, Song Y, Trivedi BK, Larsen SD, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Sekerke C, Auerbach B, Pavlovsky A, Harris MS, Bainbridge G, Caspers N Bioorg Med Chem Lett. 2007 Aug 15;17(16):4531-7. Epub 2007 Jun 6. PMID:17574411 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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