3bgl: Difference between revisions

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[[Image:3bgl.jpg|left|200px]]
[[Image:3bgl.jpg|left|200px]]


{{Structure
<!--
|PDB= 3bgl |SIZE=350|CAPTION= <scene name='initialview01'>3bgl</scene>, resolution 2.225&Aring;
The line below this paragraph, containing "STRUCTURE_3bgl", creates the "Structure Box" on the page.
|SITE= <scene name='pdbsite=AC1:Rid+Binding+Site+For+Residue+A+2'>AC1</scene>, <scene name='pdbsite=AC2:Rid+Binding+Site+For+Residue+B+1'>AC2</scene>, <scene name='pdbsite=AC3:Rid+Binding+Site+For+Residue+C+4'>AC3</scene> and <scene name='pdbsite=AC4:Rid+Binding+Site+For+Residue+D+3'>AC4</scene>
You may change the PDB parameter (which sets the PDB file loaded into the applet)  
|LIGAND= <scene name='pdbligand=RID:(3R,5R)-7-[2-(4-FLUOROPHENYL)-5-(1-METHYLETHYL)-4-(MORPHOLIN-4-YLSULFONYL)-3-PHENYL-1H-PYRROL-1-YL]-3,5-DIHYDROXYHEPTANOIC+ACID'>RID</scene>
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
|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>
or leave the SCENE parameter empty for the default display.
|GENE= HMGCR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
-->
|DOMAIN=
{{STRUCTURE_3bgl| PDB=3bgl  | SCENE= }}  
|RELATEDENTRY=[[2q1l|2Q1L]], [[2q6b|2Q6B]], [[2q6c|2Q6C]], [[2r4f|2R4F]]
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3bgl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3bgl OCA], [http://www.ebi.ac.uk/pdbsum/3bgl PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=3bgl RCSB]</span>
}}


'''Hepatoselectivity of Statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors'''
'''Hepatoselectivity of Statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors'''
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Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors., Park WK, Kennedy RM, Larsen SD, Miller S, Roth BD, Song Y, Steinbaugh BA, Sun K, Tait BD, Kowala MC, Trivedi BK, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu GH, Robertson A, Sekerke C, Bioorg Med Chem Lett. 2008 Feb 1;18(3):1151-6. Epub 2007 Dec 5. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18155906 18155906]
Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors., Park WK, Kennedy RM, Larsen SD, Miller S, Roth BD, Song Y, Steinbaugh BA, Sun K, Tait BD, Kowala MC, Trivedi BK, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu GH, Robertson A, Sekerke C, Bioorg Med Chem Lett. 2008 Feb 1;18(3):1151-6. Epub 2007 Dec 5. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18155906 18155906]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Hydroxymethylglutaryl-CoA reductase (NADPH)]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Finzel, B C.]]
[[Category: Finzel, B C.]]
[[Category: Park, W K.C.]]
[[Category: Park, W K.C.]]
[[Category: Pavlovsky, A.]]
[[Category: Pavlovsky, A.]]
[[Category: alternative splicing]]
[[Category: Alternative splicing]]
[[Category: cholesterol biosynthesis]]
[[Category: Cholesterol biosynthesis]]
[[Category: endoplasmic reticulum]]
[[Category: Endoplasmic reticulum]]
[[Category: glycoprotein]]
[[Category: Glycoprotein]]
[[Category: hmg-coa]]
[[Category: Hmg-coa]]
[[Category: lipid synthesis]]
[[Category: Lipid synthesis]]
[[Category: membrane]]
[[Category: Membrane]]
[[Category: nadph]]
[[Category: Nadph]]
[[Category: oxidoreductase]]
[[Category: Oxidoreductase]]
[[Category: peroxisome]]
[[Category: Peroxisome]]
[[Category: polymorphism]]
[[Category: Polymorphism]]
[[Category: statin]]
[[Category: Statin]]
[[Category: steroid biosynthesis]]
[[Category: Steroid biosynthesis]]
[[Category: transmembrane]]
[[Category: Transmembrane]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 30 13:38:36 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:26:02 2008''

Revision as of 13:38, 30 April 2008

File:3bgl.jpg

Template:STRUCTURE 3bgl

Hepatoselectivity of Statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors


OverviewOverview

4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The compounds were prepared via a [3+2] cycloaddition of a Munchnone with a sulfonamide-substituted alkyne. We identified compounds with greater selectivity for hepatocytes compared to L6-myocytes than rosuvastatin and atorvastatin. There was an inverse correlation of myocyte potencies and ClogP values. A number of analogs were effective at reducing cholesterol in acute and chronic in vivo models but they lacked sufficient chronic in vivo activity to warrant further development.

DiseaseDisease

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

About this StructureAbout this Structure

3BGL is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors., Park WK, Kennedy RM, Larsen SD, Miller S, Roth BD, Song Y, Steinbaugh BA, Sun K, Tait BD, Kowala MC, Trivedi BK, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu GH, Robertson A, Sekerke C, Bioorg Med Chem Lett. 2008 Feb 1;18(3):1151-6. Epub 2007 Dec 5. PMID:18155906 Page seeded by OCA on Wed Apr 30 13:38:36 2008

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