2g94

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[[Image:2g94.gif|left|200px]]
[[Image:2g94.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2g94 |SIZE=350|CAPTION= <scene name='initialview01'>2g94</scene>, resolution 1.86&Aring;
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The line below this paragraph, containing "STRUCTURE_2g94", 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=ZPQ:N~2~-[(2R,4S,5S)-5-{[N-{[(3,5-DIMETHYL-1H-PYRAZOL-1-YL)METHOXY]CARBONYL}-3-(METHYLSULFONYL)-L-ALANYL]AMINO}-4-HYDROXY-2,7-DIMETHYLOCTANOYL]-N-ISOBUTYL-L-VALINAMIDE'>ZPQ</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_2g94| PDB=2g94 | 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=2g94 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2g94 OCA], [http://www.ebi.ac.uk/pdbsum/2g94 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2g94 RCSB]</span>
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}}
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'''Crystal structure of beta-secretase bound to a potent and highly selective inhibitor.'''
'''Crystal structure of beta-secretase bound to a potent and highly selective inhibitor.'''
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[[Category: Hong, L.]]
[[Category: Hong, L.]]
[[Category: Tang, J.]]
[[Category: Tang, J.]]
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[[Category: alzheimer's disease]]
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[[Category: Alzheimer's disease]]
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[[Category: asp2]]
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[[Category: Asp2]]
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[[Category: aspartic protease]]
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[[Category: Aspartic protease]]
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[[Category: bace]]
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[[Category: Bace]]
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[[Category: beta secretase]]
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[[Category: Beta secretase]]
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[[Category: drug design]]
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[[Category: Drug design]]
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[[Category: memapsin]]
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[[Category: Memapsin]]
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[[Category: protease inhibitor]]
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[[Category: Protease inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:50:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:13:29 2008''
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Revision as of 01:50, 4 May 2008

Image:2g94.gif

Template:STRUCTURE 2g94

Crystal structure of beta-secretase bound to a potent and highly selective inhibitor.


Overview

Structure-based design, synthesis, and X-ray structure of protein-ligand complexes of memapsin 2 are described. The inhibitors are designed specifically to interact with S2- and S3-active site residues to provide selectivity over memapsin 1 and cathepsin D. Inhibitor 6 has exhibited exceedingly potent inhibitory activity against memapsin 2 and selectivity over memapsin 1 (>3800-fold) and cathepsin D (>2500-fold). A protein-ligand crystal structure revealed cooperative interactions in the S2- and S3-active sites of memapsin 2. These interactions may serve as an important guide to design selectivity over memapsin 1 and cathepsin D.

About this Structure

2G94 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors., Ghosh AK, Kumaragurubaran N, Hong L, Lei H, Hussain KA, Liu CF, Devasamudram T, Weerasena V, Turner R, Koelsch G, Bilcer G, Tang J, J Am Chem Soc. 2006 Apr 26;128(16):5310-1. PMID:16620080 Page seeded by OCA on Sun May 4 04:50:19 2008

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OCA

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