2zis

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{{Seed}}
 
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[[Image:2zis.jpg|left|200px]]
 
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==Crystal Structure of rat protein farnesyltransferase complexed with a bezoruran inhibitor and FPP==
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The line below this paragraph, containing "STRUCTURE_2zis", creates the "Structure Box" on the page.
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<StructureSection load='2zis' size='340' side='right'caption='[[2zis]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2zis]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ZIS OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2ZIS FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 2.6&#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=ACY:ACETIC+ACID'>ACY</scene>, <scene name='pdbligand=FPP:FARNESYL+DIPHOSPHATE'>FPP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NH8:3-{2-[(S)-(4-CYANOPHENYL)(HYDROXY)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-5-NITRO-1-BENZOFURAN-7-YL}BENZONITRILE'>NH8</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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{{STRUCTURE_2zis| PDB=2zis | SCENE= }}
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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=2zis FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2zis OCA], [https://pdbe.org/2zis PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2zis RCSB], [https://www.ebi.ac.uk/pdbsum/2zis PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2zis ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/FNTA_RAT FNTA_RAT] Catalyzes the transfer of a farnesyl or geranyl-geranyl moiety from farnesyl or geranyl-geranyl pyrophosphate to a cysteine at the fourth position from the C-terminus of several proteins having the C-terminal sequence Cys-aliphatic-aliphatic-X. The alpha subunit is thought to participate in a stable complex with the substrate. The beta subunit binds the peptide substrate. Through RAC1 prenylation and activation may positively regulate neuromuscular junction development downstream of MUSK (By similarity).
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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/zi/2zis_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=2zis ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice.
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===Crystal Structure of rat protein farnesyltransferase complexed with a bezoruran inhibitor and FPP===
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Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.,Asoh K, Kohchi M, Hyoudoh I, Ohtsuka T, Masubuchi M, Kawasaki K, Ebiike H, Shiratori Y, Fukami TA, Kondoh O, Tsukaguchi T, Ishii N, Aoki Y, Shimma N, Sakaitani M Bioorg Med Chem Lett. 2009 Mar 15;19(6):1753-7. Epub 2009 Feb 11. PMID:19217288<ref>PMID:19217288</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 2zis" style="background-color:#fffaf0;"></div>
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==About this Structure==
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==See Also==
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2ZIS is a 2 chains structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ZIS OCA].
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*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
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[[Category: Protein farnesyltransferase]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Fukami, T A.]]
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[[Category: Fukami TA]]
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[[Category: Ishii, N.]]
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[[Category: Ishii N]]
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[[Category: Kondoh, O.]]
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[[Category: Kondoh O]]
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[[Category: Nagata, Y.]]
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[[Category: Nagata Y]]
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[[Category: Sogabe, S.]]
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[[Category: Sogabe S]]
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[[Category: Metal-binding]]
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[[Category: Phosphoprotein]]
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[[Category: Prenyltransferase]]
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[[Category: Transferase]]
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[[Category: Zinc]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 25 09:21:49 2009''
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Current revision

Crystal Structure of rat protein farnesyltransferase complexed with a bezoruran inhibitor and FPP

PDB ID 2zis

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