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[[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size="350" color="white" frame="true" align="right" spinBox="true"
caption="1nl4, resolution 2.7&Aring;" />
'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor'''<br />


==Overview==
==Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor==
A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (&lt;1nM), FTase/GGTase selective (&gt;300-fold) and cellularly active (&lt;or=80nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented.
<StructureSection load='1nl4' size='340' side='right'caption='[[1nl4]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[1nl4]] 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=1NL4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1NL4 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]] 2.7&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FTL:4-[(3-CYANO-BENZYL)-(3-METHYL-3H-IMIDAZOL-4-YLMETHYL)-AMINO]-2-NAPHTHALEN-1-YL-BENZONITRILE'>FTL</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</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=1nl4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1nl4 OCA], [https://pdbe.org/1nl4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1nl4 RCSB], [https://www.ebi.ac.uk/pdbsum/1nl4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1nl4 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/nl/1nl4_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=1nl4 ConSurf].
<div style="clear:both"></div>


==About this Structure==
==See Also==
1NL4 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=HFP:'>HFP</scene> and <scene name='pdbligand=FTL:'>FTL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NL4 OCA].
*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
 
__TOC__
==Reference==
</StructureSection>
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase., Curtin ML, Florjancic AS, Cohen J, Gu WZ, Frost DJ, Muchmore SW, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1367-71. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12657284 12657284]
[[Category: Large Structures]]
[[Category: Protein complex]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Cohen, J.]]
[[Category: Cohen J]]
[[Category: Curtin, M L.]]
[[Category: Curtin ML]]
[[Category: Florjancic, A S.]]
[[Category: Florjancic AS]]
[[Category: Frost, D J.]]
[[Category: Frost DJ]]
[[Category: Gu, W J.]]
[[Category: Gu W-J]]
[[Category: Muchmore, S W.]]
[[Category: Muchmore SW]]
[[Category: Sham, H L.]]
[[Category: Sham HL]]
[[Category: FTL]]
[[Category: HFP]]
[[Category: ZN]]
[[Category: prenyltransferase]]
[[Category: transferase]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:07:14 2008''

Latest revision as of 07:57, 14 February 2024

Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor

1nl4, resolution 2.70Å

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