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1a42

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[[Image:1a42.gif|left|200px]]
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{{STRUCTURE_1a42| PDB=1a42 | SCENE= }}
{{STRUCTURE_1a42| PDB=1a42 | SCENE= }}
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'''HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE'''
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===HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 9541386 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9541386}}
==About this Structure==
==About this Structure==
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[[Category: Lyase]]
[[Category: Lyase]]
[[Category: Zinc]]
[[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 Mon Jun 30 15:58:41 2008''

Revision as of 12:58, 30 June 2008

Image:1a42.png

Template:STRUCTURE 1a42

HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE

Template:ABSTRACT PUBMED 9541386

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

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