1n9a

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[[Image:1n9a.gif|left|200px]]
 
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==Farnesyltransferase complex with tetrahydropyridine inhibitors==
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The line below this paragraph, containing "STRUCTURE_1n9a", creates the "Structure Box" on the page.
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<StructureSection load='1n9a' size='340' side='right'caption='[[1n9a]], [[Resolution|resolution]] 3.20&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[1n9a]] 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=1N9A OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1N9A FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 3.2&#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=FTI:1-{2-[3-(4-CYANO-BENZYL)-3H-IMIDAZOL-4-YL]-ACETYL}-5-NAPHTHALEN-1-YL-1,2,3,6-TETRAHYDRO-PYRIDINE-4-CARBONITRILE'>FTI</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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{{STRUCTURE_1n9a| PDB=1n9a | SCENE= }}
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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=1n9a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1n9a OCA], [https://pdbe.org/1n9a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1n9a RCSB], [https://www.ebi.ac.uk/pdbsum/1n9a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1n9a 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/n9/1n9a_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=1n9a ConSurf].
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<div style="clear:both"></div>
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'''Farnesyltransferase complex with tetrahydropyridine 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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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 bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.
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[[Category: Large Structures]]
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==About this Structure==
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1N9A 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=1N9A OCA].
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==Reference==
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Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency., 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):1363-6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12657283 12657283]
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[[Category: Protein complex]]
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[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Cohen, J.]]
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[[Category: Cohen J]]
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[[Category: Conner, S J.O.]]
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[[Category: Gu WZ]]
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[[Category: Gu, W Z.]]
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[[Category: Gwaltney II SL]]
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[[Category: Hasvold, L.]]
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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: Imade, H.]]
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[[Category: Li Q]]
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[[Category: Li, Q.]]
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[[Category: Nelson LT]]
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[[Category: Nelson, L T.]]
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[[Category: O'Conner SJ]]
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[[Category: Sullivan, G M.]]
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[[Category: Sullivan GM]]
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[[Category: Wang, W.]]
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[[Category: Wang W]]
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[[Category: Farnesyltransferase]]
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[[Category: Prenyltransferase]]
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[[Category: Tetrahydropyridine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:15:16 2008''
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Current revision

Farnesyltransferase complex with tetrahydropyridine inhibitors

PDB ID 1n9a

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