1a42

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[[Image:1a42.gif|left|200px]]
[[Image:1a42.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1a42 |SIZE=350|CAPTION= <scene name='initialview01'>1a42</scene>, resolution 2.25&Aring;
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The line below this paragraph, containing "STRUCTURE_1a42", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=ZN:Zn+Binding+Site'>ZN</scene>
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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=BZU:(4R)-2-(2-ETHOXYETHYL)-4-(ETHYLAMINO)-3,4-DIHYDRO-2H-THIENO[3,2-E][1,2]THIAZINE-6-SULFONAMIDE+1,1-DIOXIDE'>BZU</scene>, <scene name='pdbligand=HG:MERCURY+(II)+ION'>HG</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= HUMAN CAII ([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_1a42| PDB=1a42 | 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=1a42 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1a42 OCA], [http://www.ebi.ac.uk/pdbsum/1a42 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1a42 RCSB]</span>
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}}
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'''HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE'''
'''HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE'''
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[[Category: Boriack-Sjodin, P A.]]
[[Category: Boriack-Sjodin, P A.]]
[[Category: Christianson, D W.]]
[[Category: Christianson, D W.]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: lyase]]
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[[Category: Lyase]]
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[[Category: zinc]]
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[[Category: Zinc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 09:47:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 18:32:50 2008''
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Revision as of 06:47, 2 May 2008

Image:1a42.gif

Template:STRUCTURE 1a42

HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE


Overview

Carbonic anhydrase IV (CAIV) is a membrane-associated enzyme anchored to plasma membrane surfaces by a phosphatidylinositol glycan linkage. We have determined the 2.8-angstroms resolution crystal structure of a truncated, soluble form of recombinant murine CAIV. We have also determined the structure of its complex with a drug used for glaucoma therapy, the sulfonamide inhibitor brinzolamide (Azopt). The overall structure of murine CAIV is generally similar to that of human CAIV; however, some local structural differences are found in the active site resulting from amino acid sequence differences in the "130's segment" and the residue-63 loop (these may affect the nearby catalytic proton shuttle, His-64). Similar to human CAIV, the C-terminus of murine CAIV is surrounded by a substantial electropositive surface potential that may stabilize the interaction with the phospholipid membrane. Binding interactions observed for brinzolamide rationalize the generally weaker affinity of inhibitors used in glaucoma therapy toward CAIV compared with CAII.

About this Structure

1A42 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structures of murine carbonic anhydrase IV and human carbonic anhydrase II complexed with brinzolamide: molecular basis of isozyme-drug discrimination., Stams T, Chen Y, Boriack-Sjodin PA, Hurt JD, Liao J, May JA, Dean T, Laipis P, Silverman DN, Christianson DW, Protein Sci. 1998 Mar;7(3):556-63. PMID:9541386 Page seeded by OCA on Fri May 2 09:47:00 2008

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OCA

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