7cn1: Difference between revisions

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<StructureSection load='7cn1' size='340' side='right'caption='[[7cn1]], [[Resolution|resolution]] 3.70&Aring;' scene=''>
<StructureSection load='7cn1' size='340' side='right'caption='[[7cn1]], [[Resolution|resolution]] 3.70&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[7cn1]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7CN1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7CN1 FirstGlance]. <br>
<table><tr><td colspan='2'>[[7cn1]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7CN1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7CN1 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=K:POTASSIUM+ION'>K</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.7&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=K:POTASSIUM+ION'>K</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=7cn1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7cn1 OCA], [https://pdbe.org/7cn1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7cn1 RCSB], [https://www.ebi.ac.uk/pdbsum/7cn1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7cn1 ProSAT]</span></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=7cn1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7cn1 OCA], [https://pdbe.org/7cn1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7cn1 RCSB], [https://www.ebi.ac.uk/pdbsum/7cn1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7cn1 ProSAT]</span></td></tr>
</table>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The hERG channel is a voltage-gated potassium channel involved in cardiac repolarization. Off-target hERG inhibition by drugs has become a critical issue in the pharmaceutical industry. The three-dimensional structure of the hERG channel was recently reported at 3.8-A resolution using cryogenic electron microscopy (cryo-EM). However, the drug inhibition mechanism remains unclear because of the scarce structural information regarding the drug- and potassium-bound hERG channels. In this study, we obtained the cryo-EM density map of potassium-bound hERG channel complexed with astemizole, a well-known hERG inhibitor that increases risk of potentially fatal arrhythmia, at 3.5-A resolution. The structure suggested that astemizole inhibits potassium conduction by binding directly below the selectivity filter. Furthermore, we propose a possible binding model of astemizole to the hERG channel and provide insights into the unusual sensitivity of hERG to several drugs.


Cryo-EM Structure of K(+)-Bound hERG Channel Complexed with the Blocker Astemizole.,Asai T, Adachi N, Moriya T, Oki H, Maru T, Kawasaki M, Suzuki K, Chen S, Ishii R, Yonemori K, Igaki S, Yasuda S, Ogasawara S, Senda T, Murata T Structure. 2021 Mar 4;29(3):203-212.e4. doi: 10.1016/j.str.2020.12.007. Epub 2021, Jan 14. PMID:33450182<ref>PMID:33450182</ref>
==See Also==
 
*[[Potassium channel 3D structures|Potassium channel 3D structures]]
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 7cn1" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Adachi, N]]
[[Category: Adachi N]]
[[Category: Asai, T]]
[[Category: Asai T]]
[[Category: Kawasaki, M]]
[[Category: Kawasaki M]]
[[Category: Moriya, T]]
[[Category: Moriya T]]
[[Category: Murata, T]]
[[Category: Murata T]]
[[Category: Senda, T]]
[[Category: Senda T]]
[[Category: Suzuki, K]]
[[Category: Suzuki K]]
[[Category: Potassium channel]]
[[Category: Transport protein]]

Latest revision as of 13:51, 27 March 2024

Cryo-EM structure of K+-bound hERG channel in the presence of astemizoleCryo-EM structure of K+-bound hERG channel in the presence of astemizole

Structural highlights

7cn1 is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:Electron Microscopy, Resolution 3.7Å
Ligands:
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

See Also

7cn1, resolution 3.70Å

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