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1eh4

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[[Image:1eh4.jpg|left|200px]]
 
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{{Structure
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==BINARY COMPLEX OF CASEIN KINASE-1 FROM S. POMBE WITH AN ATP COMPETITIVE INHIBITOR, IC261==
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|PDB= 1eh4 |SIZE=350|CAPTION= <scene name='initialview01'>1eh4</scene>, resolution 2.80&Aring;
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<StructureSection load='1eh4' size='340' side='right'caption='[[1eh4]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <scene name='pdbligand=IC1:3-[(2,4,6-TRIMETHOXY-PHENYL)-METHYLENE]-INDOLIN-2-ONE'>IC1</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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<table><tr><td colspan='2'>[[1eh4]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Schizosaccharomyces_pombe Schizosaccharomyces pombe]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1EH4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1EH4 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]] 2.8&#8491;</td></tr>
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|GENE=
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=IC1:3-[(2,4,6-TRIMETHOXY-PHENYL)-METHYLENE]-INDOLIN-2-ONE'>IC1</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=1eh4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1eh4 OCA], [https://pdbe.org/1eh4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1eh4 RCSB], [https://www.ebi.ac.uk/pdbsum/1eh4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1eh4 ProSAT]</span></td></tr>
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|RELATEDENTRY=[[1csn|1CSN]], [[2csn|2CSN]]
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</table>
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1eh4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1eh4 OCA], [http://www.ebi.ac.uk/pdbsum/1eh4 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1eh4 RCSB]</span>
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== Function ==
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}}
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[https://www.uniprot.org/uniprot/CKI1_SCHPO CKI1_SCHPO] Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates.
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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/eh/1eh4_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=1eh4 ConSurf].
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<div style="clear:both"></div>
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'''BINARY COMPLEX OF CASEIN KINASE-1 FROM S. POMBE WITH AN ATP COMPETITIVE INHIBITOR, IC261'''
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==See Also==
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*[[Casein kinase 3D structures|Casein kinase 3D structures]]
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__TOC__
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==Overview==
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</StructureSection>
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Members of the casein kinase-1 family of protein kinases play an essential role in cell regulation and disease pathogenesis. Unlike most protein kinases, they appear to function as constitutively active enzymes. As a result, selective pharmacological inhibitors can play an important role in dissection of casein kinase-1-dependent processes. To address this need, new small molecule inhibitors of casein kinase-1 acting through ATP-competitive and ATP-noncompetitive mechanisms were isolated on the basis of in vitro screening. Here we report the crystal structure of 3-[(2,4,6-trimethoxyphenyl) methylidenyl]-indolin-2-one (IC261), an ATP-competitive inhibitor with differential activity among casein kinase-1 isoforms, in complex with the catalytic domain of fission yeast casein kinase-1 refined to a crystallographic R-factor of 22.4% at 2.8 A resolution. The structure reveals that IC261 stabilizes casein kinase-1 in a conformation midway between nucleotide substrate liganded and nonliganded conformations. We propose that adoption of this conformation by casein kinase-1 family members stabilizes a delocalized network of side chain interactions and results in a decreased dissociation rate of inhibitor.
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[[Category: Large Structures]]
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==About this Structure==
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1EH4 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Schizosaccharomyces_pombe Schizosaccharomyces pombe]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1EH4 OCA].
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==Reference==
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Crystal structure of a conformation-selective casein kinase-1 inhibitor., Mashhoon N, DeMaggio AJ, Tereshko V, Bergmeier SC, Egli M, Hoekstra MF, Kuret J, J Biol Chem. 2000 Jun 30;275(26):20052-60. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/10749871 10749871]
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[[Category: Schizosaccharomyces pombe]]
[[Category: Schizosaccharomyces pombe]]
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[[Category: Single protein]]
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[[Category: Bergmeier SC]]
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[[Category: Bergmeier, S C.]]
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[[Category: Demaggio AJ]]
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[[Category: Demaggio, A J.]]
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[[Category: Egli M]]
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[[Category: Egli, M.]]
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[[Category: Hoekstra MF]]
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[[Category: Hoekstra, M F.]]
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[[Category: Kuret J]]
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[[Category: Kuret, J.]]
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[[Category: Mashhoon N]]
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[[Category: Mashhoon, N.]]
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[[Category: Tereshko V]]
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[[Category: Tereshko, V.]]
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[[Category: casein kinase-1]]
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[[Category: protein kinase]]
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[[Category: protein-inhibitor binary complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:02:28 2008''
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Current revision

BINARY COMPLEX OF CASEIN KINASE-1 FROM S. POMBE WITH AN ATP COMPETITIVE INHIBITOR, IC261

PDB ID 1eh4

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