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2oah

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[[Image:2oah.jpg|left|200px]]
[[Image:2oah.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2oah |SIZE=350|CAPTION= <scene name='initialview01'>2oah</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_2oah", 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=QIN:N-[(1S,2S)-2-AMINO-1-(3-THIENYLMETHYL)HEXYL]-2-({[(1S,2S)-2-METHYLCYCLOPROPYL]METHYL}AMINO)-6-[METHYL(METHYLSULFONYL)AMINO]ISONICOTINAMIDE'>QIN</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_2oah| PDB=2oah | 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=2oah FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oah OCA], [http://www.ebi.ac.uk/pdbsum/2oah PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oah 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 10:31:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:15:03 2008''
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Revision as of 07:31, 4 May 2008

Image:2oah.jpg

Template:STRUCTURE 2oah

Crystal Structure of Human Beta Secretase Complexed with inhibitor


Overview

A series of low-molecular weight 2,6-diamino-isonicotinamide BACE-1 inhibitors containing an amine transition-state isostere were synthesized and shown to be highly potent in both enzymatic and cell-based assays. These inhibitors contain a trans-S,S-methyl cyclopropane P(3) which bind BACE-1 in a 10s-loop down conformation giving rise to highly potent compounds with favorable molecular weight and moderate to high susceptibility to P-glycoprotein (P-gp) efflux.

About this Structure

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

Reference

Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation., Stauffer SR, Stanton MG, Gregro AR, Steinbeiser MA, Shaffer JR, Nantermet PG, Barrow JC, Rittle KE, Collusi D, Espeseth AS, Lai MT, Pietrak BL, Holloway MK, McGaughey GB, Munshi SK, Hochman JH, Simon AJ, Selnick HG, Graham SL, Vacca JP, Bioorg Med Chem Lett. 2007 Mar 15;17(6):1788-92. Epub 2006 Dec 21. PMID:17257835 Page seeded by OCA on Sun May 4 10:31:22 2008

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