1ni1

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(New page: 200px<br /><applet load="1ni1" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ni1, resolution 2.30&Aring;" /> '''Imidazole and cyanop...)
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[[Image:1ni1.gif|left|200px]]<br /><applet load="1ni1" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="1ni1, resolution 2.30&Aring;" />
 
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'''Imidazole and cyanophenyl farnesyl transferase inhibitors'''<br />
 
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==Overview==
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==Imidazole and cyanophenyl farnesyl transferase inhibitors==
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A pyridyl moiety was introduced into a previously developed series of, farnesyltransferase inhibitors containing imidazole and cyanophenyl (such, as 4), resulting in potent inhibitors with improved pharmacokinetics.
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<StructureSection load='1ni1' size='340' side='right'caption='[[1ni1]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1ni1]] 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=1NI1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1NI1 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]] 2.3&#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=2C5:2-CHLORO-5-(3-CHLORO-PHENYL)-6-[(4-CYANO-PHENYL)-(3-METHYL-3H-IMIDAZOL-4-YL)-+METHOXYMETHYL]-NICOTINONITRILE'>2C5</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=1ni1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ni1 OCA], [https://pdbe.org/1ni1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1ni1 RCSB], [https://www.ebi.ac.uk/pdbsum/1ni1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1ni1 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/ni/1ni1_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=1ni1 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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1NI1 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 ZN, HFP and 2C5 as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1NI1 OCA].
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*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
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__TOC__
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==Reference==
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</StructureSection>
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Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability., Tong Y, Lin NH, Wang L, Hasvold L, Wang W, Leonard N, Li T, Li Q, Cohen J, Gu WZ, Zhang H, Stoll V, Bauch J, Marsh K, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 May 5;13(9):1571-4. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12699757 12699757]
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[[Category: Large Structures]]
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[[Category: Protein complex]]
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[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Bauch, J.]]
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[[Category: Bauch J]]
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[[Category: Cohen, J.]]
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[[Category: Cohen J]]
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[[Category: Gu, W.Z.]]
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[[Category: Gu WZ]]
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[[Category: Hasvold, L.]]
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[[Category: Hasvold L]]
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[[Category: Leonard, N.]]
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[[Category: Leonard N]]
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[[Category: Li, Q.]]
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[[Category: Li Q]]
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[[Category: Li, T.]]
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[[Category: Li T]]
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[[Category: Lin, N.H.]]
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[[Category: Lin NH]]
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[[Category: Marsh, K.]]
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[[Category: Marsh K]]
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[[Category: Rosenberg, S.H.]]
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[[Category: Rosenberg SH]]
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[[Category: Sham, H.L.]]
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[[Category: Sham HL]]
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[[Category: Stoll, V.]]
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[[Category: Stoll V]]
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[[Category: Tong, Y.]]
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[[Category: Tong Y]]
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[[Category: Wang, L.]]
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[[Category: Wang L]]
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[[Category: Wang, W.]]
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[[Category: Wang W]]
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[[Category: Zhang, H.]]
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[[Category: Zhang H]]
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[[Category: 2C5]]
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[[Category: HFP]]
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[[Category: ZN]]
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[[Category: cyanophenyl]]
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[[Category: ftase]]
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[[Category: prenyltransferase]]
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[[Category: transferase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 22:16:36 2007''
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Current revision

Imidazole and cyanophenyl farnesyl transferase inhibitors

PDB ID 1ni1

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