4g28

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==Calcium-calmodulin complexed with the calmodulin binding domain from a small conductance potassium channel splice variant and EBIO-1==
==Calcium-calmodulin complexed with the calmodulin binding domain from a small conductance potassium channel splice variant and EBIO-1==
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<StructureSection load='4g28' size='340' side='right' caption='[[4g28]], [[Resolution|resolution]] 1.63&Aring;' scene=''>
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<StructureSection load='4g28' size='340' side='right'caption='[[4g28]], [[Resolution|resolution]] 1.63&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4g28]] 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=4G28 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4G28 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4g28]] 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=4G28 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4G28 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0W8:1-ETHYL-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE'>0W8</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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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]] 1.63&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3sjq|3sjq]], [[1g4y|1g4y]], [[4g27|4g27]]</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=0W8:1-ETHYL-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE'>0W8</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Kcnn2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus]), Calm1, Calm, Cam, Cam1, Calm2, Cam2, Camb, Calm3, Cam3, Camc ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])</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=4g28 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g28 OCA], [https://pdbe.org/4g28 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4g28 RCSB], [https://www.ebi.ac.uk/pdbsum/4g28 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4g28 ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4g28 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g28 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4g28 RCSB], [http://www.ebi.ac.uk/pdbsum/4g28 PDBsum]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/KCNN2_RAT KCNN2_RAT]] Forms a voltage-independent potassium channel activated by intracellular calcium. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization. The channel is blocked by apamin.
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[https://www.uniprot.org/uniprot/KCNN2_RAT KCNN2_RAT] Forms a voltage-independent potassium channel activated by intracellular calcium. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization. The channel is blocked by apamin.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Small- and intermediate-conductance Ca(2+)-activated potassium channels, activated by Ca(2+)-bound calmodulin, have an important role in regulating membrane excitability. These channels are also linked to clinical abnormalities. A tremendous amount of effort has been devoted to developing small molecule compounds targeting these channels. However, these compounds often suffer from low potency and lack of selectivity, hindering their potential for clinical use. A key contributing factor is the lack of knowledge of the binding site(s) for these compounds. Here we demonstrate by X-ray crystallography that the binding pocket for the compounds of the 1-ethyl-2-benzimidazolinone (1-EBIO) class is located at the calmodulin-channel interface. We show that, based on structure data and molecular docking, mutations of the channel can effectively change the potency of these compounds. Our results provide insight into the molecular nature of the binding pocket and its contribution to the potency and selectivity of the compounds of the 1-EBIO class.
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Identification of the functional binding pocket for compounds targeting small-conductance Ca(2+)-activated potassium channels.,Zhang M, Pascal JM, Schumann M, Armen RS, Zhang JF Nat Commun. 2012 Aug 28;3:1021. doi: 10.1038/ncomms2017. PMID:22929778<ref>PMID:22929778</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==See Also==
==See Also==
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*[[Calmodulin|Calmodulin]]
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*[[Calmodulin 3D structures|Calmodulin 3D structures]]
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*[[Potassium Channel|Potassium Channel]]
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*[[Potassium channel 3D structures|Potassium channel 3D structures]]
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== References ==
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<references/>
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Large Structures]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Pascal, J M]]
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[[Category: Pascal JM]]
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[[Category: Zhang, J F]]
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[[Category: Zhang J-F]]
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[[Category: Zhang, M]]
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[[Category: Zhang M]]
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[[Category: Ef hand]]
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[[Category: Metal binding protein]]
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[[Category: Metal transport-calcium binding protein complex]]
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[[Category: Protein-protein complex]]
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Current revision

Calcium-calmodulin complexed with the calmodulin binding domain from a small conductance potassium channel splice variant and EBIO-1

PDB ID 4g28

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