3b92

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[[Image:3b92.jpg|left|200px]]
[[Image:3b92.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 3b92 |SIZE=350|CAPTION= <scene name='initialview01'>3b92</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_3b92", 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=440:3-{[4-(BUT-2-YN-1-YLOXY)PHENYL]SULFONYL}PROPANE-1-THIOL'>440</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_3b92| PDB=3b92 | 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=3b92 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3b92 OCA], [http://www.ebi.ac.uk/pdbsum/3b92 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=3b92 RCSB]</span>
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}}
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'''Novel thio-based TACE inhibitors Part 2: Rational design, synthesis and SAR of thiol-contaning aryl sufones'''
'''Novel thio-based TACE inhibitors Part 2: Rational design, synthesis and SAR of thiol-contaning aryl sufones'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Wei, Y.]]
[[Category: Wei, Y.]]
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[[Category: alternative splicing]]
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[[Category: Alternative splicing]]
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[[Category: aryl-sulfonamide]]
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[[Category: Aryl-sulfonamide]]
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[[Category: cleavage on pair of basic residue]]
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[[Category: Cleavage on pair of basic residue]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: membrane]]
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[[Category: Membrane]]
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[[Category: metal-binding]]
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[[Category: Metal-binding]]
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[[Category: metalloprotease]]
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[[Category: Metalloprotease]]
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[[Category: notch signaling pathway]]
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[[Category: Notch signaling pathway]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: sh3-binding]]
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[[Category: Sh3-binding]]
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[[Category: tace inhibitor]]
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[[Category: Tace inhibitor]]
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[[Category: tnf-alpha converting enzyme]]
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[[Category: Tnf-alpha converting enzyme]]
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[[Category: transmembrane]]
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[[Category: Transmembrane]]
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[[Category: zinc]]
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[[Category: Zinc]]
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[[Category: zymogen]]
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[[Category: Zymogen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 30 13:36:51 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:24:15 2008''
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Revision as of 10:36, 30 April 2008

Image:3b92.jpg

Template:STRUCTURE 3b92

Novel thio-based TACE inhibitors Part 2: Rational design, synthesis and SAR of thiol-contaning aryl sufones


Overview

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

About this Structure

3B92 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones., Bandarage UK, Wang T, Come JH, Perola E, Wei Y, Rao BG, Bioorg Med Chem Lett. 2008 Jan 1;18(1):44-8. Epub 2007 Nov 13. PMID:18054488 Page seeded by OCA on Wed Apr 30 13:36:51 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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