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==Structure of SUR1 in complex with mitiglinide== | |||
<StructureSection load='7wit' size='340' side='right'caption='[[7wit]], [[Resolution|resolution]] 3.21Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[7wit]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [https://en.wikipedia.org/wiki/Mesocricetus_auratus Mesocricetus auratus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7WIT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7WIT FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9I0:(2S)-4-[(3aR,7aS)-1,3,3a,4,5,6,7,7a-octahydroisoindol-2-yl]-4-oxidanylidene-2-(phenylmethyl)butanoic+acid'>9I0</scene>, <scene name='pdbligand=ATP:ADENOSINE-5-TRIPHOSPHATE'>ATP</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=7wit FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7wit OCA], [https://pdbe.org/7wit PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7wit RCSB], [https://www.ebi.ac.uk/pdbsum/7wit PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7wit ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/A0A1U8CME7_MESAU A0A1U8CME7_MESAU] [https://www.uniprot.org/uniprot/A2VDS4_BOVIN A2VDS4_BOVIN] | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Mitiglinide is a highly selective fast-acting anti-diabetic drug that induces insulin secretion by inhibiting pancreatic KATP channels. However, how mitiglinide binds KATP channels remains unknown. Here, we show the cryo-EM structure of the SUR1 subunit complexed with mitiglinide. The structure reveals that mitiglinide binds inside the common insulin secretagogue-binding site of SUR1, which is surrounded by TM7, TM8, TM16, and TM17. Mitiglinide locks SUR1 in the NBD-separated inward-facing conformation. The detailed structural analysis of the mitiglinide-binding site uncovers the molecular basis of its high selectivity. | |||
Structural Insights Into the High Selectivity of the Anti-Diabetic Drug Mitiglinide.,Wang M, Wu JX, Chen L Front Pharmacol. 2022 Jun 30;13:929684. doi: 10.3389/fphar.2022.929684., eCollection 2022. PMID:35847046<ref>PMID:35847046</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
<div class="pdbe-citations 7wit" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Bos taurus]] | |||
[[Category: Large Structures]] | |||
[[Category: Mesocricetus auratus]] | |||
[[Category: Chen L]] | |||
[[Category: Wang MM]] | |||
Latest revision as of 23:07, 16 November 2022
Structure of SUR1 in complex with mitiglinideStructure of SUR1 in complex with mitiglinide
Structural highlights
FunctionPublication Abstract from PubMedMitiglinide is a highly selective fast-acting anti-diabetic drug that induces insulin secretion by inhibiting pancreatic KATP channels. However, how mitiglinide binds KATP channels remains unknown. Here, we show the cryo-EM structure of the SUR1 subunit complexed with mitiglinide. The structure reveals that mitiglinide binds inside the common insulin secretagogue-binding site of SUR1, which is surrounded by TM7, TM8, TM16, and TM17. Mitiglinide locks SUR1 in the NBD-separated inward-facing conformation. The detailed structural analysis of the mitiglinide-binding site uncovers the molecular basis of its high selectivity. Structural Insights Into the High Selectivity of the Anti-Diabetic Drug Mitiglinide.,Wang M, Wu JX, Chen L Front Pharmacol. 2022 Jun 30;13:929684. doi: 10.3389/fphar.2022.929684., eCollection 2022. PMID:35847046[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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