2vj8

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[[Image:2vj8.jpg|left|200px]]
[[Image:2vj8.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2vj8 |SIZE=350|CAPTION= <scene name='initialview01'>2vj8</scene>, resolution 1.8&Aring;
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The line below this paragraph, containing "STRUCTURE_2vj8", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Zn+Binding+Site+For+Chain+A'>AC1</scene>, <scene name='pdbsite=AC2:Yb+Binding+Site+For+Chain+A'>AC2</scene>, <scene name='pdbsite=AC3:Yb+Binding+Site+For+Chain+A'>AC3</scene>, <scene name='pdbsite=AC4:Yb+Binding+Site+For+Chain+A'>AC4</scene>, <scene name='pdbsite=AC5:Imd+Binding+Site+For+Chain+A'>AC5</scene>, <scene name='pdbsite=AC6:Act+Binding+Site+For+Chain+A'>AC6</scene> and <scene name='pdbsite=AC7:Ha2+Binding+Site+For+Chain+A'>AC7</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=HA2:6-[{(2S)-2-AMINO-3-[4-(BENZYLOXY)PHENYL]PROPYL}(HYDROXY)AMINO]-6-OXOHEXANOIC+ACID)'>HA2</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Leukotriene-A(4)_hydrolase Leukotriene-A(4) hydrolase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.3.2.6 3.3.2.6] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2vj8| PDB=2vj8 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2vj8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vj8 OCA], [http://www.ebi.ac.uk/pdbsum/2vj8 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2vj8 RCSB]</span>
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}}
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'''COMPLEX OF HUMAN LEUKOTRIENE A4 HYDROLASE WITH A HYDROXAMIC ACID INHIBITOR'''
'''COMPLEX OF HUMAN LEUKOTRIENE A4 HYDROLASE WITH A HYDROXAMIC ACID INHIBITOR'''
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Crystal structures of leukotriene A4 hydrolase in complex with captopril and two competitive tight-binding inhibitors., Thunnissen MM, Andersson B, Samuelsson B, Wong CH, Haeggstrom JZ, FASEB J. 2002 Oct;16(12):1648-50. Epub 2002 Aug 7. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12207002 12207002]
Crystal structures of leukotriene A4 hydrolase in complex with captopril and two competitive tight-binding inhibitors., Thunnissen MM, Andersson B, Samuelsson B, Wong CH, Haeggstrom JZ, FASEB J. 2002 Oct;16(12):1648-50. Epub 2002 Aug 7. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12207002 12207002]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Leukotriene-A(4) hydrolase]]
 
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Andersson, B.]]
[[Category: Andersson, B.]]
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[[Category: Thunnissen, M M.G M.]]
[[Category: Thunnissen, M M.G M.]]
[[Category: Wong, C H.]]
[[Category: Wong, C H.]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: hydroxamic acid]]
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[[Category: Hydroxamic acid]]
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[[Category: leukotriene hydrolase]]
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[[Category: Leukotriene hydrolase]]
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[[Category: metalloprotease]]
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[[Category: Metalloprotease]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: zinc]]
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[[Category: Zinc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:55:27 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:13:04 2008''
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Revision as of 15:55, 4 May 2008

Image:2vj8.jpg

Template:STRUCTURE 2vj8

COMPLEX OF HUMAN LEUKOTRIENE A4 HYDROLASE WITH A HYDROXAMIC ACID INHIBITOR


Overview

Leukotriene (LT) A4 hydrolase/aminopeptidase is a bifunctional zinc enzyme that catalyzes the final step in the biosynthesis of LTB4, a potent chemoattractant and immune modulating lipid mediator. Here, we report a high-resolution crystal structure of LTA4 hydrolase in complex with captopril, a classical inhibitor of the zinc peptidase angiotensin-converting enzyme. Captopril makes few interactions with the protein, but its free thiol group is bound to the zinc, apparently accounting for most of its inhibitory action on LTA4 hydrolase. In addition, we have determined the structures of LTA4 hydrolase in complex with two selective tight-binding inhibitors, a thioamine and a hydroxamic acid. Their common benzyloxyphenyl tail, designed to mimic the carbon backbone of LTA4, binds into a narrow hydrophobic cavity in the protein. The free hydroxyl group of the hydroxamic acid makes a suboptimal, monodentate complex with the zinc, and strategies for improved inhibitor design can be deduced from the structure. Taken together, the three crystal structures provide the molecular basis for the divergent pharmacological profiles of LTA4 hydrolase inhibitors. Moreover, they help define the binding pocket for the fatty acid-derived epoxide LTA4 as well as the subsites for a tripeptide substrate, which in turn have important implications for the molecular mechanisms of enzyme catalyses.

About this Structure

2VJ8 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Crystal structures of leukotriene A4 hydrolase in complex with captopril and two competitive tight-binding inhibitors., Thunnissen MM, Andersson B, Samuelsson B, Wong CH, Haeggstrom JZ, FASEB J. 2002 Oct;16(12):1648-50. Epub 2002 Aug 7. PMID:12207002 Page seeded by OCA on Sun May 4 18:55:27 2008

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