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==Structure of human Leukotriene A4 hydrolase in complex with inhibitor 4AZ==
==Structure of human Leukotriene A4 hydrolase in complex with inhibitor 4AZ==
<StructureSection load='5bpp' size='340' side='right' caption='[[5bpp]], [[Resolution|resolution]] 2.03&Aring;' scene=''>
<StructureSection load='5bpp' size='340' side='right'caption='[[5bpp]], [[Resolution|resolution]] 2.03&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[5bpp]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5BPP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5BPP FirstGlance]. <br>
<table><tr><td colspan='2'>[[5bpp]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5BPP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5BPP FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=A4Z:2-(4-BUTOXYPHENYL)-N-HYDROXYACETAMIDE'>A4Z</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.03&#8491;</td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5aen|5aen]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A4Z:2-(4-BUTOXYPHENYL)-N-HYDROXYACETAMIDE'>A4Z</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=YB:YTTERBIUM+(III)+ION'>YB</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><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></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5bpp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5bpp OCA], [https://pdbe.org/5bpp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5bpp RCSB], [https://www.ebi.ac.uk/pdbsum/5bpp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5bpp ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5bpp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5bpp OCA], [http://pdbe.org/5bpp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5bpp RCSB], [http://www.ebi.ac.uk/pdbsum/5bpp PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5bpp ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/LKHA4_HUMAN LKHA4_HUMAN]] Epoxide hydrolase that catalyzes the final step in the biosynthesis of the proinflammatory mediator leukotriene B4. Has also aminopeptidase activity.<ref>PMID:1897988</ref> <ref>PMID:1975494</ref> <ref>PMID:2244921</ref> <ref>PMID:12207002</ref> <ref>PMID:11917124</ref> <ref>PMID:15078870</ref> <ref>PMID:18804029</ref>
[https://www.uniprot.org/uniprot/LKHA4_HUMAN LKHA4_HUMAN] Epoxide hydrolase that catalyzes the final step in the biosynthesis of the proinflammatory mediator leukotriene B4. Has also aminopeptidase activity.<ref>PMID:1897988</ref> <ref>PMID:1975494</ref> <ref>PMID:2244921</ref> <ref>PMID:12207002</ref> <ref>PMID:11917124</ref> <ref>PMID:15078870</ref> <ref>PMID:18804029</ref>  
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Neutrophils play an important role in the occurrence and development of acute lung injury (ALI). Leukotriene B4 (LTB4), a hydrolysis product of epoxide leukotriene A4 (LTA4) catalyzed by LTA4 hydrolase (LTA4H), is one of the most potent chemoattractants for neutrophil. Bufexamac is a drug widely used as an anti-inflammatory agent on the skin, however, the mechanism of action is still not fully understood. In this study, we found bufexamac was capable of specifically inhibiting LTA4H enzymatic activity and revealed the mode of interaction of bufexamac and LTA4H using X-ray crystallography. Moreover, bufexamac significantly prevented the production of LTB4 in neutrophil and inhibited the fMLP-induced neutrophil migration through inhibition of LTA4H. Finally, bufexamac significantly attenuated lung inflammation as reflected by reduced LTB4 levels and weakened neutrophil infiltration in bronchoalveolar lavage fluid from a lipopolysaccharide-induced ALI mouse model. In summary, our study indicates that bufexamac acts as an inhibitor of LTB4 biosynthesis and may have potential clinical applications for the treatment of ALI.


Bufexamac ameliorates LPS-induced acute lung injury in mice by targeting LTA4H.,Xiao Q, Dong N, Yao X, Wu D, Lu Y, Mao F, Zhu J, Li J, Huang J, Chen A, Huang L, Wang X, Yang G, He G, Xu Y, Lu W Sci Rep. 2016 Apr 29;6:25298. doi: 10.1038/srep25298. PMID:27126280<ref>PMID:27126280</ref>
==See Also==
 
*[[Leukotriene A4 Hydrolase|Leukotriene A4 Hydrolase]]
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 5bpp" style="background-color:#fffaf0;"></div>
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Dong, N N]]
[[Category: Homo sapiens]]
[[Category: Huang, J]]
[[Category: Large Structures]]
[[Category: Lu, W Q]]
[[Category: Dong NN]]
[[Category: Ou, P Y]]
[[Category: Huang J]]
[[Category: Wu, D]]
[[Category: Lu WQ]]
[[Category: Xiao, Q]]
[[Category: Ou PY]]
[[Category: Complex]]
[[Category: Wu D]]
[[Category: Enzyme]]
[[Category: Xiao Q]]
[[Category: Hydrolase-hydrolase inhibitor complex]]
[[Category: Inflammation]]
[[Category: Inhibitor]]

Latest revision as of 09:07, 20 March 2024

Structure of human Leukotriene A4 hydrolase in complex with inhibitor 4AZ

5bpp, resolution 2.03Å

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