3otq

<StructureSection load='3otq' size='340' side='right' caption='[[3otq]], [[Resolution|resolution]] 3.00&Aring;' scene=''>

<table><tr><td colspan='2'>[[3otq]] is a 1 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=3OTQ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3OTQ FirstGlance]. <br>

</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MZL:N-[4-(5-ETHYL-3-PYRIDIN-3-YL-1H-PYRAZOL-1-YL)PHENYL]PYRIDINE-3-CARBOXAMIDE'>MZL</scene></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=3otq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3otq OCA], [http://pdbe.org/3otq PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3otq RCSB], [http://www.ebi.ac.uk/pdbsum/3otq PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3otq ProSAT]</span></td></tr>

== Function ==

[[http://www.uniprot.org/uniprot/HYES_HUMAN HYES_HUMAN]] Bifunctional enzyme. The C-terminal domain has epoxide hydrolase activity and acts on epoxides (alkene oxides, oxiranes) and arene oxides. Plays a role in xenobiotic metabolism by degrading potentially toxic epoxides. Also determines steady-state levels of physiological mediators. The N-terminal domain has lipid phosphatase activity, with the highest activity towards threo-9,10-phosphonooxy-hydroxy-octadecanoic acid, followed by erythro-9,10-phosphonooxy-hydroxy-octadecanoic acid, 12-phosphonooxy-octadec-9Z-enoic acid, 12-phosphonooxy-octadec-9E-enoic acid, and p-nitrophenyl phospate.<ref>PMID:12574508</ref> <ref>PMID:12574510</ref>

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== Publication Abstract from PubMed ==

A novel series of pyrazole sEH inhibitors is reported. Lead optimization efforts to replace the aniline core are also described. In particular, 2-pyridine, 3-pyridine and pyridazine analogs are potent sEH inhibitors with favorable CYP3A4 inhibitory and microsomal stability profiles.

Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain.,Lo HY, Man CC, Fleck RW, Farrow NA, Ingraham RH, Kukulka A, Proudfoot JR, Betageri R, Kirrane T, Patel U, Sharma R, Hoermann MA, Kabcenell A, Lombaert SD Bioorg Med Chem Lett. 2010 Nov 15;20(22):6379-83. Epub 2010 Sep 19. PMID:20934334<ref>PMID:20934334</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 3otq" style="background-color:#fffaf0;"></div>

*[[Epoxide hydrolase|Epoxide hydrolase]]

[[Category: Human]]

[[Category: Soluble epoxide hydrolase]]

[[Category: Farrow, N A]]

[[Category: Hydrolase]]