1n94

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(New page: 200px<br /><applet load="1n94" size="450" color="white" frame="true" align="right" spinBox="true" caption="1n94, resolution 3.50&Aring;" /> '''Aryl Tetrahydropyrid...)
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[[Image:1n94.gif|left|200px]]<br /><applet load="1n94" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="1n94, resolution 3.50&Aring;" />
 
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'''Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates'''<br />
 
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==Overview==
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==Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates==
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Inhibitors of farnesyltransferase are effective against a variety of, tumors in mouse models of cancer. Clinical trials to evaluate these agents, in humans are ongoing. In our effort to develop new farnesyltransferase, inhibitors, we have discovered a series of aryl tetrahydropyridines that, incorporate substituted glycine, phenylalanine and histidine residues. The, design, synthesis, SAR and biological properties of these compounds will, be discussed.
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<StructureSection load='1n94' size='340' side='right'caption='[[1n94]], [[Resolution|resolution]] 3.50&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1n94]] 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=1N94 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1N94 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]] 3.5&#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=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=TIN:2-{(5-{[BUTYL-(2-CYCLOHEXYL-ETHYL)-AMINO]-METHYL}-2-METHYL-BIPHENYL-2-CARBONYL)-AMINO]-4-METHYLSULFANYL-BUTYRIC+ACID'>TIN</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=1n94 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1n94 OCA], [https://pdbe.org/1n94 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1n94 RCSB], [https://www.ebi.ac.uk/pdbsum/1n94 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1n94 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/FNTB_RAT FNTB_RAT] Catalyzes the transfer of a farnesyl moiety from farnesyl pyrophosphate to a cysteine at the fourth position from the C-terminus of several proteins. The beta subunit is responsible for peptide-binding.
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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/n9/1n94_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.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=1n94 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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Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.
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==About this Structure==
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Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.,Gwaltney SL 2nd, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, Sham HL Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62. PMID:12657282<ref>PMID:12657282</ref>
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1N94 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 TIN as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1N94 OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives., Gwaltney SL 2nd, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12657282 12657282]
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</div>
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[[Category: Protein complex]]
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<div class="pdbe-citations 1n94" style="background-color:#fffaf0;"></div>
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[[Category: Rattus norvegicus]]
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[[Category: Cohen, J.]]
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[[Category: Connor, S.J.O.]]
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[[Category: Gu, W.Z.]]
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[[Category: Hasvold, L.]]
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[[Category: II, S.L.Gwaltney.]]
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[[Category: Imade, H.]]
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[[Category: Li, Q.]]
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[[Category: Nelson, L.T.]]
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[[Category: Sullivan, G.M.]]
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[[Category: Wang, W.]]
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[[Category: HFP]]
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[[Category: TIN]]
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[[Category: ZN]]
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[[Category: farnesyltransferase]]
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[[Category: prenyltransferase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 22:04:02 2007''
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==See Also==
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*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
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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]]
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[[Category: Rattus norvegicus]]
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[[Category: Cohen J]]
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[[Category: Gu WZ]]
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[[Category: Gwaltney II SL]]
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[[Category: Hasvold L]]
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[[Category: Imade H]]
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[[Category: Li Q]]
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[[Category: Nelson LT]]
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[[Category: O'Connor SJ]]
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[[Category: Sullivan GM]]
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[[Category: Wang W]]

Current revision

Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates

PDB ID 1n94

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