2ph6

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[[Image:2ph6.jpg|left|200px]]
[[Image:2ph6.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2ph6 |SIZE=350|CAPTION= <scene name='initialview01'>2ph6</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2ph6", 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=712:3-({[(1R)-1-(4-FLUOROPHENYL)ETHYL]AMINO}CARBONYL)-5-[METHYL(METHYLSULFONYL)AMINO]BENZYL+ALPHA-METHYL-D-PHENYLALANINATE'>712</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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= BACE1, BACE ([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_2ph6| PDB=2ph6 | SCENE= }}
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|RELATEDENTRY=[[1tqf|1TQF]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ph6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ph6 OCA], [http://www.ebi.ac.uk/pdbsum/2ph6 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ph6 RCSB]</span>
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}}
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'''Crystal Structure of Human Beta Secretase Complexed with inhibitor'''
'''Crystal Structure of Human Beta Secretase Complexed with inhibitor'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Munshi, S.]]
[[Category: Munshi, S.]]
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[[Category: aspartyl protease]]
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[[Category: Aspartyl protease]]
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[[Category: bace]]
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[[Category: Bace]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 13:06:10 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:35:51 2008''
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Revision as of 10:06, 4 May 2008

Image:2ph6.jpg

Template:STRUCTURE 2ph6

Crystal Structure of Human Beta Secretase Complexed with inhibitor


Overview

This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the beta-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability.

About this Structure

2PH6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors., Lindsley SR, Moore KP, Rajapakse HA, Selnick HG, Young MB, Zhu H, Munshi S, Kuo L, McGaughey GB, Colussi D, Crouthamel MC, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Simon AJ, Seabrook GR, Hazuda DJ, Pudvah NT, Hochman JH, Graham SL, Vacca JP, Nantermet PG, Bioorg Med Chem Lett. 2007 Jul 15;17(14):4057-61. Epub 2007 Apr 27. PMID:17482814 Page seeded by OCA on Sun May 4 13:06:10 2008

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OCA

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