1a42: Difference between revisions
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:1a42.gif|left|200px]]<br /><applet load="1a42" size=" | [[Image:1a42.gif|left|200px]]<br /><applet load="1a42" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="1a42, resolution 2.25Å" /> | caption="1a42, resolution 2.25Å" /> | ||
'''HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE'''<br /> | '''HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE'''<br /> | ||
| Line 10: | Line 10: | ||
==About this Structure== | ==About this Structure== | ||
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] Known structural/functional Site: <scene name='pdbsite=ZN:Zn Binding Site'>ZN</scene>. Full crystallographic information is available from [http:// | 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 <scene name='pdbligand=HG:'>HG</scene>, <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=BZU:'>BZU</scene> 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] Known structural/functional Site: <scene name='pdbsite=ZN:Zn+Binding+Site'>ZN</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1A42 OCA]. | ||
==Reference== | ==Reference== | ||
| Line 26: | Line 26: | ||
[[Category: zinc]] | [[Category: zinc]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 09:28:56 2008'' | ||
Revision as of 10:28, 3 February 2008
|
HUMAN CARBONIC ANHYDRASE II COMPLEXED WITH BRINZOLAMIDE
OverviewOverview
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.
DiseaseDisease
Known disease associated with this structure: Osteopetrosis, autosomal recessive 3, with renal tubular acidosis OMIM:[611492]
About this StructureAbout this Structure
1A42 is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Carbonate dehydratase, with EC number 4.2.1.1 Known structural/functional Site: . Full crystallographic information is available from OCA.
ReferenceReference
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 Sun Feb 3 09:28:56 2008