6jb3: Difference between revisions
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==Structure of SUR1 subunit bound with repaglinide== | |||
<StructureSection load='6jb3' size='340' side='right'caption='[[6jb3]], [[Resolution|resolution]] 3.00Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[6jb3]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6JB3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6JB3 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AJP:Digitonin'>AJP</scene>, <scene name='pdbligand=BJX:Repaglinide'>BJX</scene></td></tr> | |||
<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=6jb3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6jb3 OCA], [http://pdbe.org/6jb3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6jb3 RCSB], [http://www.ebi.ac.uk/pdbsum/6jb3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6jb3 ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Repaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. It boosts insulin secretion by inhibiting the pancreatic ATP-sensitive potassium channel (KATP). However, the mechanisms by which RPG binds to the KATP channel are poorly understood. Here, we describe two cryo-EM structures: the pancreatic KATP channel in complex with inhibitory RPG and adenosine-5'-(gamma-thio)-triphosphate (ATPgammaS) at 3.3 A and a medium-resolution structure of a RPG-bound mini SUR1 protein in which the N terminus of the inward-rectifying potassium channel 6.1 (Kir6.1) is fused to the ABC transporter module of the sulfonylurea receptor 1 (SUR1). These structures reveal the binding site of RPG in the SUR1 subunit. Furthermore, the high-resolution structure reveals the complex architecture of the ATP binding site, which is formed by both Kir6.2 and SUR1 subunits, and the domain-domain interaction interfaces. | |||
The Structural Basis for the Binding of Repaglinide to the Pancreatic KATP Channel.,Ding D, Wang M, Wu JX, Kang Y, Chen L Cell Rep. 2019 May 7;27(6):1848-1857.e4. doi: 10.1016/j.celrep.2019.04.050. PMID:31067468<ref>PMID:31067468</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
<div class="pdbe-citations 6jb3" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Large Structures]] | |||
[[Category: Chen, L]] | |||
[[Category: Ding, D]] | |||
[[Category: Kang, Y]] | |||
[[Category: Wang, M]] | |||
[[Category: Wu, J X]] | |||
[[Category: Abc transporter]] | |||
[[Category: Channel]] | |||
[[Category: Diabetes]] | |||
[[Category: Insulin secretagogue]] | |||
[[Category: Katp]] | |||
[[Category: Kir]] | |||
[[Category: Membrane protein]] | |||
[[Category: Repaglinide]] | |||
[[Category: Sur]] | |||
Revision as of 09:50, 23 May 2019
Structure of SUR1 subunit bound with repaglinideStructure of SUR1 subunit bound with repaglinide
Structural highlights
Publication Abstract from PubMedRepaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. It boosts insulin secretion by inhibiting the pancreatic ATP-sensitive potassium channel (KATP). However, the mechanisms by which RPG binds to the KATP channel are poorly understood. Here, we describe two cryo-EM structures: the pancreatic KATP channel in complex with inhibitory RPG and adenosine-5'-(gamma-thio)-triphosphate (ATPgammaS) at 3.3 A and a medium-resolution structure of a RPG-bound mini SUR1 protein in which the N terminus of the inward-rectifying potassium channel 6.1 (Kir6.1) is fused to the ABC transporter module of the sulfonylurea receptor 1 (SUR1). These structures reveal the binding site of RPG in the SUR1 subunit. Furthermore, the high-resolution structure reveals the complex architecture of the ATP binding site, which is formed by both Kir6.2 and SUR1 subunits, and the domain-domain interaction interfaces. The Structural Basis for the Binding of Repaglinide to the Pancreatic KATP Channel.,Ding D, Wang M, Wu JX, Kang Y, Chen L Cell Rep. 2019 May 7;27(6):1848-1857.e4. doi: 10.1016/j.celrep.2019.04.050. PMID:31067468[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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