1rgb
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(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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Revision as of 23:27, 20 November 2007
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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 ELD 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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