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1eqh

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[[Image:1eqh.gif|left|200px]]
 
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{{Structure
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==THE 2.7 ANGSTROM MODEL OF OVINE COX-1 COMPLEXED WITH FLURBIPROFEN==
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|PDB= 1eqh |SIZE=350|CAPTION= <scene name='initialview01'>1eqh</scene>, resolution 2.70&Aring;
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<StructureSection load='1eqh' size='340' side='right'caption='[[1eqh]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=BOG:B-OCTYLGLUCOSIDE'>BOG</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene> and <scene name='pdbligand=FLP:FLURBIPROFEN'>FLP</scene>
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<table><tr><td colspan='2'>[[1eqh]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Ovis_aries Ovis aries]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1EQH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1EQH FirstGlance]. <br>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Prostaglandin-endoperoxide_synthase Prostaglandin-endoperoxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.99.1 1.14.99.1]
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.7&#8491;</td></tr>
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|GENE=
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BOG:B-OCTYLGLUCOSIDE'>BOG</scene>, <scene name='pdbligand=FLP:FLURBIPROFEN'>FLP</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>
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}}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1eqh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1eqh OCA], [https://pdbe.org/1eqh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1eqh RCSB], [https://www.ebi.ac.uk/pdbsum/1eqh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1eqh ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PGH1_SHEEP PGH1_SHEEP] May play an important role in regulating or promoting cell proliferation in some normal and neoplastically transformed cells.
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/eq/1eqh_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1eqh ConSurf].
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<div style="clear:both"></div>
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'''THE 2.7 ANGSTROM MODEL OF OVINE COX-1 COMPLEXED WITH FLURBIPROFEN'''
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==See Also==
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*[[Cyclooxygenase 3D structures|Cyclooxygenase 3D structures]]
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__TOC__
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==Overview==
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</StructureSection>
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Nonsteroidal antiinflammatory drugs (NSAIDs) block prostanoid biosynthesis by inhibiting prostaglandin H(2) synthase (EC 1.14.99.1). NSAIDs are either rapidly reversible competitive inhibitors or slow tight-binding inhibitors of this enzyme. These different modes of inhibition correlate with clinically important differences in isoform selectivity. Hypotheses have been advanced to explain the different inhibition kinetics, but no structural data have been available to test them. We present here crystal structures of prostaglandin H(2) synthase-1 in complex with the inhibitors ibuprofen, methyl flurbiprofen, flurbiprofen, and alclofenac at resolutions ranging from 2.6 to 2.75 A. These structures allow direct comparison of enzyme complexes with reversible competitive inhibitors (ibuprofen and methyl flurbiprofen) and slow tight-binding inhibitors (alclofenac and flurbiprofen). The four inhibitors bind to the same site and adopt similar conformations. In all four complexes, the enzyme structure is essentially unchanged, exhibiting only minimal differences in the inhibitor binding site. These results argue strongly against hypotheses that explain the difference between slow tight-binding and fast reversible competitive inhibition by invoking global conformational differences or different inhibitor binding sites. Instead, they suggest that the different apparent modes of NSAID binding may result from differences in the speed and efficiency with which inhibitors can perturb the hydrogen bonding network around Arg-120 and Tyr-355.
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[[Category: Large Structures]]
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==About this Structure==
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1EQH is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Ovis_aries Ovis aries]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1EQH OCA].
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==Reference==
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Structural analysis of NSAID binding by prostaglandin H2 synthase: time-dependent and time-independent inhibitors elicit identical enzyme conformations., Selinsky BS, Gupta K, Sharkey CT, Loll PJ, Biochemistry. 2001 May 1;40(17):5172-80. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11318639 11318639]
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[[Category: Ovis aries]]
[[Category: Ovis aries]]
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[[Category: Prostaglandin-endoperoxide synthase]]
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[[Category: Gupta K]]
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[[Category: Single protein]]
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[[Category: Loll PJ]]
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[[Category: Gupta, K.]]
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[[Category: Selinsky BS]]
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[[Category: Loll, P J.]]
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[[Category: Sharkey CT]]
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[[Category: Selinsky, B S.]]
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[[Category: Sharkey, C T.]]
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[[Category: BOG]]
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[[Category: FLP]]
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[[Category: HEM]]
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[[Category: NAG]]
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[[Category: cyclooxygenase]]
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[[Category: dioxygenase]]
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[[Category: egf domain]]
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[[Category: flurbiprofen]]
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[[Category: membrane-binding domain]]
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[[Category: nsaid binding]]
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[[Category: oxidoreductase]]
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[[Category: peroxidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 10:59:03 2008''
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Current revision

THE 2.7 ANGSTROM MODEL OF OVINE COX-1 COMPLEXED WITH FLURBIPROFEN

PDB ID 1eqh

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