1pge: Difference between revisions

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New page: left|200px<br /> <applet load="1pge" size="450" color="white" frame="true" align="right" spinBox="true" caption="1pge, resolution 3.5Å" /> '''PROSTAGLANDIN H2 SYN...
 
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[[Image:1pge.gif|left|200px]]<br />
<applet load="1pge" size="450" color="white" frame="true" align="right" spinBox="true"
caption="1pge, resolution 3.5&Aring;" />
'''PROSTAGLANDIN H2 SYNTHASE-1 COMPLEXED WITH P-(2'-IODO-5'-THENOYL)HYDROTROPIC ACID (IODOSUPROFEN)'''<br />


==Overview==
==PROSTAGLANDIN H2 SYNTHASE-1 COMPLEXED WITH P-(2'-IODO-5'-THENOYL)HYDROTROPIC ACID (IODOSUPROFEN)==
The cyclooxygenase activity of the membrane protein prostaglandin H2, synthase isoform 1 (PGHS-1) is the target of the nonsteroidal, antiinflammatory drugs (NSAIDs). The X-ray crystal structures of PGHS-1 in, complex with the NSAIDs flurbiprofen and bromoaspirin have been determined, previously [Picot, D., et al. (1994) Nature 367, 243-249; Loll, P. J., et, al. (1995) Nat. Struct. Biol. 2, 637-643]. We report here the preparation, and characterization of novel potent iodinated analogs of the NSAIDs, indomethacin and suprofen, as well as the refined X-ray crystal structures, of their complexes with PGHS-1. The PGHS-iodosuprofen complex structure, has been refined at 3.5 A to an R-value of 0.189 and shows the suprofen, analog to share a common mode of binding with flurbiprofen. The, ... [[http://ispc.weizmann.ac.il/pmbin/getpm?8652509 (full description)]]
<StructureSection load='1pge' size='340' side='right'caption='[[1pge]], [[Resolution|resolution]] 3.50&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[1pge]] 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=1PGE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1PGE FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.5&#8491;</td></tr>
<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=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=ISF:P-(2-IODO-5-THENOYL)HYDROTROPIC+ACID'>ISF</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></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=1pge FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pge OCA], [https://pdbe.org/1pge PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1pge RCSB], [https://www.ebi.ac.uk/pdbsum/1pge PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1pge ProSAT]</span></td></tr>
</table>
== Function ==
[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.
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/pg/1pge_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</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=1pge ConSurf].
<div style="clear:both"></div>


==About this Structure==
==See Also==
1PGE is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Ovis_aries Ovis aries]] with NAG, BOG, HEM and ISF as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.99.1 1.14.99.1]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1PGE OCA]].
*[[Cyclooxygenase 3D structures|Cyclooxygenase 3D structures]]
 
__TOC__
==Reference==
</StructureSection>
Synthesis and use of iodinated nonsteroidal antiinflammatory drug analogs as crystallographic probes of the prostaglandin H2 synthase cyclooxygenase active site., Loll PJ, Picot D, Ekabo O, Garavito RM, Biochemistry. 1996 Jun 11;35(23):7330-40. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=8652509 8652509]
[[Category: Large Structures]]
[[Category: Ovis aries]]
[[Category: Ovis aries]]
[[Category: Single protein]]
[[Category: Garavito RM]]
[[Category: Garavito, R.M.]]
[[Category: Loll PJ]]
[[Category: Loll, P.J.]]
[[Category: Picot D]]
[[Category: Picot, D.]]
[[Category: BOG]]
[[Category: HEM]]
[[Category: ISF]]
[[Category: NAG]]
[[Category: dioxygenase]]
[[Category: oxidoreductase]]
[[Category: peroxidase]]
 
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Oct 29 16:57:08 2007''

Latest revision as of 08:55, 17 April 2024

PROSTAGLANDIN H2 SYNTHASE-1 COMPLEXED WITH P-(2'-IODO-5'-THENOYL)HYDROTROPIC ACID (IODOSUPROFEN)PROSTAGLANDIN H2 SYNTHASE-1 COMPLEXED WITH P-(2'-IODO-5'-THENOYL)HYDROTROPIC ACID (IODOSUPROFEN)

Structural highlights

1pge is a 2 chain structure with sequence from Ovis aries. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 3.5Å
Ligands:, , ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

PGH1_SHEEP May play an important role in regulating or promoting cell proliferation in some normal and neoplastically transformed cells.

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

See Also

1pge, resolution 3.50Å

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