2hkk
From Proteopedia
(New page: 200px<br /> <applet load="2hkk" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hkk, resolution 1.90Å" /> '''Carbonic anhydrase ...) |
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| - | [[Image:2hkk. | + | [[Image:2hkk.jpg|left|200px]]<br /><applet load="2hkk" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2hkk" size=" | + | |
caption="2hkk, resolution 1.90Å" /> | caption="2hkk, resolution 1.90Å" /> | ||
'''Carbonic anhydrase activators: Solution and X-ray crystallography for the interaction of andrenaline with various carbonic anhydrase isoforms'''<br /> | '''Carbonic anhydrase activators: Solution and X-ray crystallography for the interaction of andrenaline with various carbonic anhydrase isoforms'''<br /> | ||
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==Overview== | ==Overview== | ||
The activation of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), with L-adrenaline and histamine has been investigated by kinetic and X-ray, crystallographic studies. L-Adrenaline behaves as a potent activator of, isozyme CA I (activation constant of 90 nM), being a much weaker activator, of isozyme CA II (activation constant of 96 microM). Isoforms CA IV, VA, VII, and XIV were activated by L-adrenaline with K(A)s in the range of, 36-63 microM. The X-ray crystal structure of the CA II-L-adrenaline adduct, revealed that the activator plugs the entrance of the active site cavity, obstructing it almost completely. | The activation of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), with L-adrenaline and histamine has been investigated by kinetic and X-ray, crystallographic studies. L-Adrenaline behaves as a potent activator of, isozyme CA I (activation constant of 90 nM), being a much weaker activator, of isozyme CA II (activation constant of 96 microM). Isoforms CA IV, VA, VII, and XIV were activated by L-adrenaline with K(A)s in the range of, 36-63 microM. The X-ray crystal structure of the CA II-L-adrenaline adduct, revealed that the activator plugs the entrance of the active site cavity, obstructing it almost completely. | ||
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| - | ==Disease== | ||
| - | Known disease associated with this structure: Osteopetrosis, autosomal recessive 3, with renal tubular acidosis OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=611492 611492]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 2HKK 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 ZN, HG and ALE 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] Full crystallographic information is available from [http:// | + | 2HKK 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=ZN:'>ZN</scene>, <scene name='pdbligand=HG:'>HG</scene> and <scene name='pdbligand=ALE:'>ALE</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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HKK OCA]. |
==Reference== | ==Reference== | ||
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[[Category: crystal structure]] | [[Category: crystal structure]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 15:11:30 2008'' |
Revision as of 13:11, 23 January 2008
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Carbonic anhydrase activators: Solution and X-ray crystallography for the interaction of andrenaline with various carbonic anhydrase isoforms
Overview
The activation of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), with L-adrenaline and histamine has been investigated by kinetic and X-ray, crystallographic studies. L-Adrenaline behaves as a potent activator of, isozyme CA I (activation constant of 90 nM), being a much weaker activator, of isozyme CA II (activation constant of 96 microM). Isoforms CA IV, VA, VII, and XIV were activated by L-adrenaline with K(A)s in the range of, 36-63 microM. The X-ray crystal structure of the CA II-L-adrenaline adduct, revealed that the activator plugs the entrance of the active site cavity, obstructing it almost completely.
About this Structure
2HKK 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 Full crystallographic information is available from OCA.
Reference
Carbonic anhydrase activators: L-Adrenaline plugs the active site entrance of isozyme II, activating better isoforms I, IV, VA, VII, and XIV., Temperini C, Innocenti A, Scozzafava A, Mastrolorenzo A, Supuran CT, Bioorg Med Chem Lett. 2007 Feb 1;17(3):628-35. Epub 2006 Nov 15. PMID:17127057
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