1a42
From Proteopedia
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==Overview== | ==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, .. | + | 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== | ==About this Structure== | ||
| - | 1A42 is a | + | 1A42 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with HG, ZN and BZU as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Structure known Active Site: ZN. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1A42 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: zinc]] | [[Category: zinc]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 13:28:32 2007'' |
Revision as of 11:23, 5 November 2007
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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 with HG, ZN and BZU as ligands. Active as Carbonate dehydratase, with EC number 4.2.1.1 Structure known Active Site: ZN. 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 Mon Nov 5 13:28:32 2007
Categories: Carbonate dehydratase | Homo sapiens | Single protein | Boriack-Sjodin, P.A. | Christianson, D.W. | BZU | HG | ZN | Inhibitor | Lyase | Zinc
