2q1l

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[[Image:2q1l.jpg|left|200px]]
[[Image:2q1l.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2q1l |SIZE=350|CAPTION= <scene name='initialview01'>2q1l</scene>, resolution 2.050&Aring;
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The line below this paragraph, containing "STRUCTURE_2q1l", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=882:(3R,5R)-7-[5-(ANILINOCARBONYL)-3,4-BIS(4-FLUOROPHENYL)-1-ISOPROPYL-1H-PYRROL-2-YL]-3,5-DIHYDROXYHEPTANOIC+ACID'>882</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <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>
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or leave the SCENE parameter empty for the default display.
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|GENE= HMGCR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2q1l| PDB=2q1l | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2q1l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q1l OCA], [http://www.ebi.ac.uk/pdbsum/2q1l PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2q1l RCSB]</span>
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}}
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'''Design and Synthesis of Pyrrole-based, Hepatoselective HMG-CoA Reductase Inhibitors'''
'''Design and Synthesis of Pyrrole-based, Hepatoselective HMG-CoA Reductase Inhibitors'''
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Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors., Pfefferkorn JA, Song Y, Sun KL, Miller SR, Trivedi BK, Choi C, Sorenson RJ, Bratton LD, Unangst PC, Larsen SD, Poel TJ, Cheng XM, Lee C, Erasga N, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Olsen K, Mertz T, Sekerke C, Pavlovsky A, Harris MS, Bainbridge G, Caspers N, Chen H, Eberstadt M, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4538-44. Epub 2007 Jun 6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17574412 17574412]
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors., Pfefferkorn JA, Song Y, Sun KL, Miller SR, Trivedi BK, Choi C, Sorenson RJ, Bratton LD, Unangst PC, Larsen SD, Poel TJ, Cheng XM, Lee C, Erasga N, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Olsen K, Mertz T, Sekerke C, Pavlovsky A, Harris MS, Bainbridge G, Caspers N, Chen H, Eberstadt M, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4538-44. Epub 2007 Jun 6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17574412 17574412]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Hydroxymethylglutaryl-CoA reductase (NADPH)]]
 
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Finzel, B C.]]
[[Category: Finzel, B C.]]
[[Category: Harris, M S.]]
[[Category: Harris, M S.]]
[[Category: Pavlovsky, A.]]
[[Category: Pavlovsky, A.]]
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[[Category: Pfefferkorn, J A.,]]
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[[Category: Pfefferkorn, J A.]]
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[[Category: cholesterol biosynthesis]]
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[[Category: Cholesterol biosynthesis]]
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[[Category: hmg-coa]]
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[[Category: Hmg-coa]]
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[[Category: nadph]]
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[[Category: Nadph]]
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[[Category: oxidoreductase]]
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[[Category: Oxidoreductase]]
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[[Category: statin]]
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[[Category: Statin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:10:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:43:24 2008''
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Revision as of 11:10, 4 May 2008

Image:2q1l.jpg

Template:STRUCTURE 2q1l

Design and Synthesis of Pyrrole-based, Hepatoselective HMG-CoA Reductase Inhibitors


Contents

Overview

This manuscript describes the design and synthesis of a series of pyrrole-based inhibitors of HMG-CoA reductase for the treatment of hypercholesterolemia. Analogs were optimized using structure-based design and physical property considerations resulting in the identification of 44, a hepatoselective HMG-CoA reductase inhibitor with excellent acute and chronic efficacy in a pre-clinical animal models.

Disease

Known disease associated with this structure: Statins, attenuated cholesterol lowering by OMIM:[142910]

About this Structure

2Q1L is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors., Pfefferkorn JA, Song Y, Sun KL, Miller SR, Trivedi BK, Choi C, Sorenson RJ, Bratton LD, Unangst PC, Larsen SD, Poel TJ, Cheng XM, Lee C, Erasga N, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Olsen K, Mertz T, Sekerke C, Pavlovsky A, Harris MS, Bainbridge G, Caspers N, Chen H, Eberstadt M, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4538-44. Epub 2007 Jun 6. PMID:17574412 Page seeded by OCA on Sun May 4 14:10:23 2008

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OCA

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