6ncf

<table><tr><td colspan='2'>[[6ncf]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6NCF OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6NCF FirstGlance]. <br>

</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AF7:(3alpha,8alpha,17alpha,18alpha)-3-(acetyloxy)-11-oxours-12-en-23-oic+acid'>AF7</scene>, <scene name='pdbligand=FE2:FE+(II)+ION'>FE2</scene></td></tr>

<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Arachidonate_5-lipoxygenase Arachidonate 5-lipoxygenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.13.11.34 1.13.11.34] </span></td></tr>

<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6ncf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ncf OCA], [http://pdbe.org/6ncf PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6ncf RCSB], [http://www.ebi.ac.uk/pdbsum/6ncf PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6ncf ProSAT]</span></td></tr>

== Function ==

[[http://www.uniprot.org/uniprot/LOX5_HUMAN LOX5_HUMAN]] Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.<ref>PMID:21233389</ref>

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== Publication Abstract from PubMed ==

Leukotrienes (LT) are lipid mediators of the inflammatory response that are linked to asthma and atherosclerosis. LT biosynthesis is initiated by 5-lipoxygenase (5-LOX) with the assistance of the substrate-binding 5-LOX-activating protein at the nuclear membrane. Here, we contrast the structural and functional consequences of the binding of two natural product inhibitors of 5-LOX. The redox-type inhibitor nordihydroguaiaretic acid (NDGA) is lodged in the 5-LOX active site, now fully exposed by disordering of the helix that caps it in the apo-enzyme. In contrast, the allosteric inhibitor 3-acetyl-11-keto-beta-boswellic acid (AKBA) from frankincense wedges between the membrane-binding and catalytic domains of 5-LOX, some 30 A from the catalytic iron. While enzyme inhibition by NDGA is robust, AKBA promotes a shift in the regiospecificity, evident in human embryonic kidney 293 cells and in primary immune cells expressing 5-LOX. Our results suggest a new approach to isoform-specific 5-LOX inhibitor development through exploitation of an allosteric site in 5-LOX.

Structural and mechanistic insights into 5-lipoxygenase inhibition by natural products.,Gilbert NC, Gerstmeier J, Schexnaydre EE, Borner F, Garscha U, Neau DB, Werz O, Newcomer ME Nat Chem Biol. 2020 May 11. pii: 10.1038/s41589-020-0544-7. doi:, 10.1038/s41589-020-0544-7. PMID:32393899<ref>PMID:32393899</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>

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<div class="pdbe-citations 6ncf" style="background-color:#fffaf0;"></div>

== References ==

<references/>

[[Category: Arachidonate 5-lipoxygenase]]

[[Category: Human]]

[[Category: Gilbert, N C]]

[[Category: Neau, D B]]

[[Category: Newcomer, M E]]

[[Category: Oxidoreductase-oxidoreductase inhibitor complex]]