1rqi

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(New page: 200px<br /><applet load="1rqi" size="450" color="white" frame="true" align="right" spinBox="true" caption="1rqi, resolution 2.42&Aring;" /> '''Active Conformation ...)
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[[Image:1rqi.gif|left|200px]]<br /><applet load="1rqi" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="1rqi, resolution 2.42&Aring;" />
 
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'''Active Conformation of Farnesyl Pyrophosphate Synthase Bound to Isopentyl Pyrophosphate and Dimethylallyl S-Thiolodiphosphate'''<br />
 
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==Overview==
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==Active Conformation of Farnesyl Pyrophosphate Synthase Bound to Isopentyl Pyrophosphate and Dimethylallyl S-Thiolodiphosphate==
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Farnesyl pyrophosphate synthetase (FPPS) synthesizes farnesyl, pyrophosphate through successive condensations of isopentyl pyrophosphate, with dimethylallyl pyrophosphate and geranyl pyrophosphate., Nitrogen-containing bisphosphonate drugs used to treat osteoclast-mediated, bone resorption and tumor-induced hypercalcemia are potent inhibitors of, the enzyme. Here we present crystal structures of substrate and, bisphosphonate complexes of FPPS. The structures reveal how enzyme, conformational changes organize conserved active site residues to exploit, metal-induced ionization and substrate positioning for catalysis. The, structures further demonstrate how nitrogen-containing bisphosphonates, mimic a carbocation intermediate to inhibit the enzyme. Together, these, FPPS complexes provide a structural template for the design of novel, inhibitors that may prove useful for the treatment of osteoporosis and, other clinical indications including cancer.
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<StructureSection load='1rqi' size='340' side='right'caption='[[1rqi]], [[Resolution|resolution]] 2.42&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1rqi]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RQI OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1RQI FirstGlance]. <br>
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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]] 2.42&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DPO:DIPHOSPHATE'>DPO</scene>, <scene name='pdbligand=DST:DIMETHYLALLYL+S-THIOLODIPHOSPHATE'>DST</scene>, <scene name='pdbligand=IPR:ISOPENTYL+PYROPHOSPHATE'>IPR</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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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=1rqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1rqi OCA], [https://pdbe.org/1rqi PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1rqi RCSB], [https://www.ebi.ac.uk/pdbsum/1rqi PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1rqi ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/ISPA_ECOLI ISPA_ECOLI]
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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/rq/1rqi_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=1rqi ConSurf].
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<div style="clear:both"></div>
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==About this Structure==
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==See Also==
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1RQI is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] with MG, DST, IPR and DPO as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Geranyltranstransferase Geranyltranstransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.10 2.5.1.10] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1RQI OCA].
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*[[Farnesyl diphosphate synthase 3D structures|Farnesyl diphosphate synthase 3D structures]]
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__TOC__
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==Reference==
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</StructureSection>
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Structural basis for bisphosphonate-mediated inhibition of isoprenoid biosynthesis., Hosfield DJ, Zhang Y, Dougan DR, Broun A, Tari LW, Swanson RV, Finn J, J Biol Chem. 2004 Mar 5;279(10):8526-9. Epub 2003 Dec 12. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=14672944 14672944]
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[[Category: Escherichia coli]]
[[Category: Escherichia coli]]
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[[Category: Geranyltranstransferase]]
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[[Category: Large Structures]]
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[[Category: Single protein]]
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[[Category: Brooun A]]
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[[Category: Brooun, A.]]
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[[Category: Dougan DR]]
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[[Category: Dougan, D.R.]]
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[[Category: Finn J]]
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[[Category: Finn, J.]]
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[[Category: Hosfield DJ]]
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[[Category: Hosfield, D.J.]]
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[[Category: Swanson RV]]
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[[Category: Swanson, R.V.]]
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[[Category: Tari LW]]
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[[Category: Tari, L.W.]]
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[[Category: Zhang Y]]
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[[Category: Zhang, Y.]]
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[[Category: DPO]]
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[[Category: DST]]
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[[Category: IPR]]
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[[Category: MG]]
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[[Category: isoprenyl synthase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 01:47:55 2007''
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Current revision

Active Conformation of Farnesyl Pyrophosphate Synthase Bound to Isopentyl Pyrophosphate and Dimethylallyl S-Thiolodiphosphate

PDB ID 1rqi

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