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1zxc

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[[Image:1zxc.gif|left|200px]]
[[Image:1zxc.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1zxc |SIZE=350|CAPTION= <scene name='initialview01'>1zxc</scene>, resolution 2.28&Aring;
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The line below this paragraph, containing "STRUCTURE_1zxc", 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=IH6:(3S)-4-{[4-(BUT-2-YNYLOXY)PHENYL]SULFONYL}-N-HYDROXY-2,2-DIMETHYLTHIOMORPHOLINE-3-CARBOXAMIDE'>IH6</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= ADAM17, CSVP, 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_1zxc| PDB=1zxc | SCENE= }}
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|RELATEDENTRY=[[1bkc|1bkc]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1zxc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1zxc OCA], [http://www.ebi.ac.uk/pdbsum/1zxc PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1zxc RCSB]</span>
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}}
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'''Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor'''
'''Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor'''
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[[Category: Xu, W.]]
[[Category: Xu, W.]]
[[Category: Zhang, Y.]]
[[Category: Zhang, Y.]]
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[[Category: tace-inhibitor complex]]
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[[Category: Tace-inhibitor complex]]
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[[Category: tace/adam-17]]
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[[Category: Tace/adam-17]]
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[[Category: zn-endopeptidase]]
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[[Category: Zn-endopeptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 18:11:47 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:42:54 2008''
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Revision as of 15:11, 3 May 2008

Image:1zxc.gif

Template:STRUCTURE 1zxc

Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor


Overview

The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1' group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model.

About this Structure

1ZXC is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates., Levin JI, Chen JM, Laakso LM, Du M, Du X, Venkatesan AM, Sandanayaka V, Zask A, Xu J, Xu W, Zhang Y, Skotnicki JS, Bioorg Med Chem Lett. 2005 Oct 1;15(19):4345-9. PMID:16084720 Page seeded by OCA on Sat May 3 18:11:47 2008

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