2oi0

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[[Image:2oi0.jpg|left|200px]]
[[Image:2oi0.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2oi0 |SIZE=350|CAPTION= <scene name='initialview01'>2oi0</scene>, resolution 2.000&Aring;
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The line below this paragraph, containing "STRUCTURE_2oi0", 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=283:(3S)-1-{[4-(BUT-2-YN-1-YLOXY)PHENYL]SULFONYL}PYRROLIDINE-3-THIOL'>283</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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/ADAM_17_endopeptidase ADAM 17 endopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.86 3.4.24.86] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= TACE ([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_2oi0| PDB=2oi0 | 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=2oi0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oi0 OCA], [http://www.ebi.ac.uk/pdbsum/2oi0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oi0 RCSB]</span>
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}}
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'''Crystal structure analysis 0f the TNF-a Coverting Enzyme (TACE) in complexed with Aryl-sulfonamide'''
'''Crystal structure analysis 0f the TNF-a Coverting Enzyme (TACE) in complexed with Aryl-sulfonamide'''
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[[Category: Rao, G B.]]
[[Category: Rao, G B.]]
[[Category: Wei, Y.]]
[[Category: Wei, Y.]]
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[[Category: aryl-sulfonamide]]
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[[Category: Aryl-sulfonamide]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: tace inhibitor]]
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[[Category: Tace inhibitor]]
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[[Category: tnf-a coverting enzyme]]
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[[Category: Tnf-a coverting enzyme]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:57:56 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:18:13 2008''
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Revision as of 07:57, 4 May 2008

Image:2oi0.jpg

Template:STRUCTURE 2oi0

Crystal structure analysis 0f the TNF-a Coverting Enzyme (TACE) in complexed with Aryl-sulfonamide


Overview

A series of potent thiol-containing aryl sulfonamide TACE inhibitors was designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 4b has shown excellent in vitro potency against the isolated TACE enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 4b bound to TACE was obtained.

About this Structure

2OI0 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides., Govinda Rao B, Bandarage UK, Wang T, Come JH, Perola E, Wei Y, Tian SK, Saunders JO, Bioorg Med Chem Lett. 2007 Apr 15;17(8):2250-3. Epub 2007 Jan 26. PMID:17289381 Page seeded by OCA on Sun May 4 10:57:56 2008

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OCA

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