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2fix

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[[Image:2fix.gif|left|200px]]
[[Image:2fix.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2fix |SIZE=350|CAPTION= <scene name='initialview01'>2fix</scene>, resolution 3.50&Aring;
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The line below this paragraph, containing "STRUCTURE_2fix", 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=870:N-[7-(3-AMINOPHENYL)-5-METHOXY-1,3-BENZOXAZOL-2-YL]-2,5-DICHLOROBENZENESULFONAMIDE'>870</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/Fructose-bisphosphatase Fructose-bisphosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.11 3.1.3.11] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2fix| PDB=2fix | SCENE= }}
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|RELATEDENTRY=[[2fhy|2fhy]], [[2fie|2fie]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2fix FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fix OCA], [http://www.ebi.ac.uk/pdbsum/2fix PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2fix RCSB]</span>
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}}
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'''Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitiors'''
'''Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitiors'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Abad-Zapatero, C.]]
[[Category: Abad-Zapatero, C.]]
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[[Category: allosteric inhibitors human liver fbpase]]
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[[Category: Allosteric inhibitors human liver fbpase]]
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[[Category: benzoxazole]]
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[[Category: Benzoxazole]]
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[[Category: intersubunit allosteric inhibitors of human liver fbpase]]
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[[Category: Intersubunit allosteric inhibitors of human liver fbpase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:57:16 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:03:22 2008''
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Revision as of 00:57, 4 May 2008

Image:2fix.gif

Template:STRUCTURE 2fix

Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitiors


Overview

A series of novel benzoxazole benzenesulfonamides was synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase-1). Extensive SAR studies led to a potent inhibitor, 53, with an IC(50) of 0.57microM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.

About this Structure

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

Reference

Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase., Lai C, Gum RJ, Daly M, Fry EH, Hutchins C, Abad-Zapatero C, von Geldern TW, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1807-10. Epub 2006 Jan 30. PMID:16446092 Page seeded by OCA on Sun May 4 03:57:16 2008

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