2q6c

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[[Image:2q6c.png|left|200px]]
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==Design and synthesis of novel, conformationally restricted HMG-COA reductase inhibitors==
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<StructureSection load='2q6c' size='340' side='right' caption='[[2q6c]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2q6c]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q6C OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2Q6C FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=HR1:(3R,5R)-7-[1-(4-FLUOROPHENYL)-3-ISOPROPYL-4-OXO-5-PHENYL-4,5-DIHYDRO-3H-PYRROLO[2,3-C]QUINOLIN-2-YL]-3,5-DIHYDROXYHEPTANOIC+ACID'>HR1</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><br>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2q1l|2q1l]], [[2q6b|2q6b]]</td></tr>
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<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">HMGCR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
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<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Hydroxymethylglutaryl-CoA_reductase_(NADPH) Hydroxymethylglutaryl-CoA reductase (NADPH)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.1.1.34 1.1.1.34] </span></td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2q6c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q6c OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2q6c RCSB], [http://www.ebi.ac.uk/pdbsum/2q6c PDBsum]</span></td></tr>
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<table>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/q6/2q6c_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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.
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{{STRUCTURE_2q6c| PDB=2q6c | SCENE= }}
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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<ref>PMID:17574411</ref>
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===Design and synthesis of novel, conformationally restricted HMG-COA reductase inhibitors===
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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{{ABSTRACT_PUBMED_17574411}}
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==About this Structure==
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[[2q6c]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q6C OCA].
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==See Also==
==See Also==
*[[HMG-CoA Reductase|HMG-CoA Reductase]]
*[[HMG-CoA Reductase|HMG-CoA Reductase]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:017574411</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Finzel, B C.]]
[[Category: Finzel, B C.]]

Revision as of 06:23, 29 September 2014

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

2q6c, resolution 2.00Å

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