1eou

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[[Image:1eou.jpg|left|200px]]
[[Image:1eou.jpg|left|200px]]
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{{Structure
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|PDB= 1eou |SIZE=350|CAPTION= <scene name='initialview01'>1eou</scene>, resolution 2.10&Aring;
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The line below this paragraph, containing "STRUCTURE_1eou", 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=SMS:SULFAMIC+ACID+2,3-O-(1-METHYLETHYLIDENE)-4,5-O-SULFONYL-BETA-FRUCTOPYRANOSE+ESTER'>SMS</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/Carbonate_dehydratase Carbonate dehydratase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.2.1.1 4.2.1.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1eou| PDB=1eou | SCENE= }}
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|RELATEDENTRY=[[1am6|1AM6]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1eou FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1eou OCA], [http://www.ebi.ac.uk/pdbsum/1eou PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1eou RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH AN ANTICONVULSANT SUGAR SULFAMATE'''
'''CRYSTAL STRUCTURE OF HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH AN ANTICONVULSANT SUGAR SULFAMATE'''
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[[Category: Maryanoff, B E.]]
[[Category: Maryanoff, B E.]]
[[Category: Recacha, R.]]
[[Category: Recacha, R.]]
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[[Category: co2 hydration]]
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[[Category: Co2 hydration]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: protein-inhibitor complex]]
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[[Category: Protein-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 15:21:33 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:06:54 2008''
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Revision as of 12:21, 2 May 2008

Image:1eou.jpg

Template:STRUCTURE 1eou

CRYSTAL STRUCTURE OF HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH AN ANTICONVULSANT SUGAR SULFAMATE


Overview

The fructose-based sugar sulphamate RWJ-37497, a potent analogue of the widely used anti-epileptic drug topiramate, possesses anti-convulsant and carbonic anhydrase-inhibitory activities. We have studied the binding interactions of RWJ-37497 in the active site of human carbonic anhydrase II by X-ray crystallography. The atomic positions of the enzyme inhibitor complex were refined at a resolution of 2.1 A (1 A=0.1 nm) to the final crystallographic R and R(free) values of 0.18 and 0.23, respectively. The inhibitor co-ordinates to the active-site zinc ion through its oxygen atom and the ionized nitrogen atom of the sulphamate group by replacing the metal-bound water molecules, although the sulphamoyl oxygen atom provides a rather lengthy co-ordination. The 4,5-cyclic sulphate group is positioned in a hydrophobic pocket of the active site, making contacts with the residues Phe-131, Leu-198, Pro-201 and Pro-202. Since the ligand was found to be intact, concerns about RWJ-37947 irreversibly alkylating the enzyme through its 4,5-cyclic sulphate group were dispelled.

About this Structure

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

Reference

Crystal structure of human carbonic anhydrase II complexed with an anti-convulsant sugar sulphamate., Recacha R, Costanzo MJ, Maryanoff BE, Chattopadhyay D, Biochem J. 2002 Feb 1;361(Pt 3):437-41. PMID:11802772 Page seeded by OCA on Fri May 2 15:21:33 2008

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