1ni1

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[[Image:1ni1.gif|left|200px]]
 
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{{Structure
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==Imidazole and cyanophenyl farnesyl transferase inhibitors==
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|PDB= 1ni1 |SIZE=350|CAPTION= <scene name='initialview01'>1ni1</scene>, resolution 2.30&Aring;
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<StructureSection load='1ni1' size='340' side='right'caption='[[1ni1]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <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>
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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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|ACTIVITY=
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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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|GENE= FNTA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus]), FNTB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])
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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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|DOMAIN=
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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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|RELATEDENTRY=[[1n9a|1N9A]], [[1n95|1N95]]
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</table>
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ni1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ni1 OCA], [http://www.ebi.ac.uk/pdbsum/1ni1 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ni1 RCSB]</span>
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== Function ==
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}}
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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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'''Imidazole and cyanophenyl farnesyl transferase inhibitors'''
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==See Also==
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*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
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__TOC__
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==Overview==
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</StructureSection>
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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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[[Category: Large Structures]]
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==About this Structure==
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1NI1 is a [[Protein complex]] 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=1NI1 OCA].
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==Reference==
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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://www.ncbi.nlm.nih.gov/pubmed/12699757 12699757]
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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: 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://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:30:39 2008''
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Current revision

Imidazole and cyanophenyl farnesyl transferase inhibitors

PDB ID 1ni1

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