View source for 2zir


==Crystal Structure of rat protein farnesyltransferase complexed with a benzofuran inhibitor and FPP==
<StructureSection load='2zir' size='340' side='right'caption='[[2zir]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2zir]] 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=2ZIR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2ZIR 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]] 2.4&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FPP:FARNESYL+DIPHOSPHATE'>FPP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NH7:2-[(S)-(4-CHLOROPHENYL)(HYDROXY)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-N-MORPHOLIN-4-YL-7-PHENYL-1-BENZOFURAN-5-CARBOXAMIDE'>NH7</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=2zir FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2zir OCA], [https://pdbe.org/2zir PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2zir RCSB], [https://www.ebi.ac.uk/pdbsum/2zir PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2zir ProSAT]</span></td></tr>
</table>
== Function ==
[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).
== 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/zi/2zir_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=2zir ConSurf].
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== Publication Abstract from PubMed ==
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.

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>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<div class="pdbe-citations 2zir" style="background-color:#fffaf0;"></div>

==See Also==
*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Large Structures]]
[[Category: Rattus norvegicus]]
[[Category: Fukami TA]]
[[Category: Ishii N]]
[[Category: Kondoh O]]
[[Category: Nagata Y]]
[[Category: Sogabe S]]