3ksq

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{{STRUCTURE_3ksq| PDB=3ksq | SCENE= }}
 
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===Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors===
 
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{{ABSTRACT_PUBMED_20056542}}
 
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==Function==
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==Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors==
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[[http://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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<StructureSection load='3ksq' size='340' side='right'caption='[[3ksq]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3ksq]] 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=3KSQ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3KSQ 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]] 2.1&#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=FPP:FARNESYL+DIPHOSPHATE'>FPP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=Z96:TERT-BUTYL+4-{(11S)-8-CHLORO-6-[(R)-HYDROXY(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-YL}PIPERAZINE-1-CARBOXYLATE'>Z96</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=3ksq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ksq OCA], [https://pdbe.org/3ksq PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3ksq RCSB], [https://www.ebi.ac.uk/pdbsum/3ksq PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3ksq 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/ks/3ksq_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=3ksq 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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The discovery of C-linked imidazole azaheptapyridine bridgehead FPT inhibitors is described. This novel class of compounds are sub nM FPT enzyme inhibitors with potent cellular inhibitory activities. This series also has reduced hERG activity versus previous N-linked imidazole series. X-ray of compound 10a bound to FTase revealed strong interaction between bridgehead imidazole 3N with catalytic zinc atom.
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==About this Structure==
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Discovery of C-imidazole azaheptapyridine FPT inhibitors.,Zhu HY, Cooper AB, Desai J, Njoroge G, Kirschmeier P, Bishop WR, Strickland C, Hruza A, Doll RJ, Girijavallabhan VM Bioorg Med Chem Lett. 2010 Feb 1;20(3):1134-6. Epub 2009 Dec 6. PMID:20056542<ref>PMID:20056542</ref>
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[[3ksq]] is a 2 chain structure with sequence 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=3KSQ 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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<ref group="xtra">PMID:020056542</ref><references group="xtra"/><references/>
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</div>
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[[Category: Protein farnesyltransferase]]
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<div class="pdbe-citations 3ksq" style="background-color:#fffaf0;"></div>
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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]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Cooper, A B.]]
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[[Category: Cooper AB]]
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[[Category: Girijavallabhan, V M.]]
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[[Category: Girijavallabhan VM]]
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[[Category: Hruza, A.]]
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[[Category: Hruza A]]
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[[Category: Kirschmeier, P.]]
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[[Category: Kirschmeier P]]
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[[Category: Njoroge, G.]]
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[[Category: Njoroge G]]
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[[Category: Strickland, C.]]
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[[Category: Strickland C]]
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[[Category: Zhu, H Y.]]
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[[Category: Zhu HY]]
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[[Category: Metal-binding]]
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[[Category: Phosphoprotein]]
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[[Category: Prenyltransferase]]
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[[Category: Transferase]]
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Current revision

Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors

PDB ID 3ksq

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