1rgb
From Proteopedia
(New page: 200px<br /><applet load="1rgb" size="450" color="white" frame="true" align="right" spinBox="true" caption="1rgb, resolution 3.30Å" /> '''Phospholipase A2 fro...) |
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| - | [[Image:1rgb.gif|left|200px]]<br /><applet load="1rgb" size=" | + | [[Image:1rgb.gif|left|200px]]<br /><applet load="1rgb" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1rgb, resolution 3.30Å" /> | caption="1rgb, resolution 3.30Å" /> | ||
'''Phospholipase A2 from Vipera ammodytes meridionalis'''<br /> | '''Phospholipase A2 from Vipera ammodytes meridionalis'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The inhibition of phospholipase A(2)s (PLA(2)s) is of pharmacological and | + | The inhibition of phospholipase A(2)s (PLA(2)s) is of pharmacological and therapeutic interest because these enzymes are involved in several inflammatory diseases. Elaidoylamide is a powerful inhibitor of a neurotoxic PLA(2) from the Vipera ammodytes meridionalis venom. The X-ray structure of the enzyme-inhibitor complex reveals a new mode of Asp49 PLA(2) inhibition by a fatty acid hydrocarbon chain. The structure contains two identical homodimers in the asymmetric unit. In each dimer one subunit is rotated by 180 degrees with respect to the other and the two molecules are oriented head-to-tail. One molecule of elaidoylamide is bound simultaneously to the substrate binding sites of two associated neurotoxic phospholipase A(2) molecules. The inhibitor binds symmetrically to the hydrophobic channels of the two monomers. The structure can be used to design anti-inflammatory drugs. |
==About this Structure== | ==About this Structure== | ||
| - | 1RGB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Vipera_ammodytes_meridionalis Vipera ammodytes meridionalis] with ELD as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Phospholipase_A(2) Phospholipase A(2)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.4 3.1.1.4] Full crystallographic information is available from [http:// | + | 1RGB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Vipera_ammodytes_meridionalis Vipera ammodytes meridionalis] with <scene name='pdbligand=ELD:'>ELD</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Phospholipase_A(2) Phospholipase A(2)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.1.4 3.1.1.4] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RGB OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Vipera ammodytes meridionalis]] | [[Category: Vipera ammodytes meridionalis]] | ||
| - | [[Category: Georgieva, D | + | [[Category: Georgieva, D N.]] |
[[Category: ELD]] | [[Category: ELD]] | ||
[[Category: elaidoylamide]] | [[Category: elaidoylamide]] | ||
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[[Category: phospholipase a2]] | [[Category: phospholipase a2]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:50:38 2008'' |
Revision as of 12:50, 21 February 2008
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Phospholipase A2 from Vipera ammodytes meridionalis
Overview
The inhibition of phospholipase A(2)s (PLA(2)s) is of pharmacological and therapeutic interest because these enzymes are involved in several inflammatory diseases. Elaidoylamide is a powerful inhibitor of a neurotoxic PLA(2) from the Vipera ammodytes meridionalis venom. The X-ray structure of the enzyme-inhibitor complex reveals a new mode of Asp49 PLA(2) inhibition by a fatty acid hydrocarbon chain. The structure contains two identical homodimers in the asymmetric unit. In each dimer one subunit is rotated by 180 degrees with respect to the other and the two molecules are oriented head-to-tail. One molecule of elaidoylamide is bound simultaneously to the substrate binding sites of two associated neurotoxic phospholipase A(2) molecules. The inhibitor binds symmetrically to the hydrophobic channels of the two monomers. The structure can be used to design anti-inflammatory drugs.
About this Structure
1RGB is a Single protein structure of sequence from Vipera ammodytes meridionalis with as ligand. Active as Phospholipase A(2), with EC number 3.1.1.4 Full crystallographic information is available from OCA.
Reference
Asp49 phospholipase A(2)-elaidoylamide complex: a new mode of inhibition., Georgieva DN, Rypniewski W, Gabdoulkhakov A, Genov N, Betzel C, Biochem Biophys Res Commun. 2004 Jul 9;319(4):1314-21. PMID:15194511
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