1x81: Difference between revisions

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New page: left|200px<br /><applet load="1x81" size="450" color="white" frame="true" align="right" spinBox="true" caption="1x81, resolution 3.5Å" /> '''Farnesyl transferase ...
 
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[[Image:1x81.gif|left|200px]]<br /><applet load="1x81" size="450" color="white" frame="true" align="right" spinBox="true"
caption="1x81, resolution 3.5&Aring;" />
'''Farnesyl transferase structure of Jansen compound'''<br />


==Overview==
==Farnesyl transferase structure of Jansen compound==
As a part of our efforts to identify potent inhibitors of, farnesyltransferase (FTase), modification of the structure of tipifarnib, through structure-based design was undertaken by replacing the, 2-quinolones with 4-quinolones and pyridones, and subsequent relocation of, the D-ring to the N-methyl group on the imidazole ring. This study has, yielded a novel series of potent and selective FTase inhibitors. The X-ray, structure of tipifarnib (1) in complex with FTase was described.
<StructureSection load='1x81' size='340' side='right'caption='[[1x81]], [[Resolution|resolution]] 3.50&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[1x81]] 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=1X81 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1X81 FirstGlance]. <br>
</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>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=JAN:6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE'>JAN</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1x81 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1x81 OCA], [https://pdbe.org/1x81 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1x81 RCSB], [https://www.ebi.ac.uk/pdbsum/1x81 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1x81 ProSAT]</span></td></tr>
</table>
== Function ==
[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).
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/x8/1x81_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</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=1x81 ConSurf].
<div style="clear:both"></div>


==About this Structure==
==See Also==
1X81 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 and JAN as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Protein_farnesyltransferase Protein farnesyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.58 2.5.1.58] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1X81 OCA].
*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
 
__TOC__
==Reference==
</StructureSection>
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors., Li Q, Claiborne A, Li T, Hasvold L, Stoll VS, Muchmore S, Jakob CG, Gu W, Cohen J, Hutchins C, Frost D, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2004 Nov 1;14(21):5367-70. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15454228 15454228]
[[Category: Large Structures]]
[[Category: Protein complex]]
[[Category: Protein farnesyltransferase]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Claiborne, A.]]
[[Category: Claiborne A]]
[[Category: Cohen, J.]]
[[Category: Cohen J]]
[[Category: Frost, D.]]
[[Category: Frost D]]
[[Category: Gu, W.]]
[[Category: Gu W]]
[[Category: Hasvold, L.]]
[[Category: Hasvold L]]
[[Category: Hutchins, C.]]
[[Category: Hutchins C]]
[[Category: Jakob, C.G.]]
[[Category: Jakob CG]]
[[Category: Li, Q.]]
[[Category: Li Q]]
[[Category: Li, T.]]
[[Category: Li T]]
[[Category: Muchmore, S.]]
[[Category: Muchmore S]]
[[Category: Rosenberg, S.H.]]
[[Category: Rosenberg SH]]
[[Category: Sham, H.L.]]
[[Category: Sham HL]]
[[Category: Stoll, V.S.]]
[[Category: Stoll VS]]
[[Category: JAN]]
[[Category: ZN]]
[[Category: fanesyltransferase]]
 
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Retrieved from "https://proteopedia.org/1x81"