2viz

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[[Image:2viz.jpg|left|200px]]
[[Image:2viz.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2viz |SIZE=350|CAPTION= <scene name='initialview01'>2viz</scene>, resolution 1.60&Aring;
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The line below this paragraph, containing "STRUCTURE_2viz", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Vg4+Binding+Site+For+Chain+A'>AC1</scene>
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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=VG4:N-[(1S,2R)-1-BENZYL-3-{[(1S)-2-(CYCLOHEXYLAMINO)-1-METHYL-2-OXOETHYL]AMINO}-2-HYDROXYPROPYL]-3-(2-OXO-2,3-DIHYDRO-1H-PYRROL-1-YL)-5-PROPOXYBENZAMIDE'>VG4</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/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2viz| PDB=2viz | SCENE= }}
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|RELATEDENTRY=[[1tqf|1TQF]], [[1xn3|1XN3]], [[1m4h|1M4H]], [[1xn2|1XN2]], [[2vie|2VIE]], [[2va6|2VA6]], [[2b8l|2B8L]], [[1ym4|1YM4]], [[2va5|2VA5]], [[1sgz|1SGZ]], [[1ujk|1UJK]], [[2b8v|2B8V]], [[1fkn|1FKN]], [[1xs7|1XS7]], [[2vij|2VIJ]], [[2va7|2VA7]], [[1ym2|1YM2]], [[1py1|1PY1]], [[1w50|1W50]], [[1ujj|1UJJ]], [[1w51|1W51]], [[2viy|2VIY]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2viz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2viz OCA], [http://www.ebi.ac.uk/pdbsum/2viz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2viz RCSB]</span>
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}}
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'''HUMAN BACE-1 IN COMPLEX WITH N-((1S,2R)-3-(((1S)-2-(CYCLOHEXYLAMINO)-1-METHYL-2-OXOETHYL)AMINO)-2-HYDROXY-1-(PHENYLMETHYL)PROPYL)-3-(2-OXO-1-PYRROLIDINYL)-5-(PROPYLOXY) BENZAMIDE'''
'''HUMAN BACE-1 IN COMPLEX WITH N-((1S,2R)-3-(((1S)-2-(CYCLOHEXYLAMINO)-1-METHYL-2-OXOETHYL)AMINO)-2-HYDROXY-1-(PHENYLMETHYL)PROPYL)-3-(2-OXO-1-PYRROLIDINYL)-5-(PROPYLOXY) BENZAMIDE'''
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[[Category: Ward, J.]]
[[Category: Ward, J.]]
[[Category: Wayne, G.]]
[[Category: Wayne, G.]]
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[[Category: alternative splicing]]
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[[Category: Alternative splicing]]
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[[Category: asp-2]]
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[[Category: Asp-2]]
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[[Category: aspartyl protease]]
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[[Category: Aspartyl protease]]
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[[Category: bace-1]]
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[[Category: Bace-1]]
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[[Category: beta-secretase]]
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[[Category: Beta-secretase]]
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[[Category: beta-site app cleaving enzyme]]
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[[Category: Beta-site app cleaving enzyme]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: memapsin-2]]
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[[Category: Memapsin-2]]
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[[Category: membrane]]
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[[Category: Membrane]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: transmembrane]]
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[[Category: Transmembrane]]
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[[Category: zymogen]]
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[[Category: Zymogen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:54:18 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:13:01 2008''
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Revision as of 15:54, 4 May 2008

Image:2viz.jpg

Template:STRUCTURE 2viz

HUMAN BACE-1 IN COMPLEX WITH N-((1S,2R)-3-(((1S)-2-(CYCLOHEXYLAMINO)-1-METHYL-2-OXOETHYL)AMINO)-2-HYDROXY-1-(PHENYLMETHYL)PROPYL)-3-(2-OXO-1-PYRROLIDINYL)-5-(PROPYLOXY) BENZAMIDE


Overview

Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of potent inhibitors based on a hydroxy ethylamine (HEA) transition-state mimetic. These inhibitors were capable of lowering amyloid production in a cell-based assay.

About this Structure

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

Reference

BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs)., Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Hawkins J, Hussain I, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Soleil V, Smith KJ, Stanway S, Stemp G, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G, Bioorg Med Chem Lett. 2008 Feb 1;18(3):1011-6. Epub 2007 Dec 15. PMID:18171614 Page seeded by OCA on Sun May 4 18:54:18 2008

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OCA

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