6jb1

From Proteopedia

(Difference between revisions)

Revision as of 08:11, 6 November 2019

Structure of pancreatic ATP-sensitive potassium channel bound with repaglinide and ATPgammaS at 3.3A resolution

Structural highlights

6jb1 is a 8 chain structure with sequence from Golden hamster and Lk3 transgenic mice. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	, , , ,
Gene:	Kcnj11 (LK3 transgenic mice), Abcc8 (Golden hamster)
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[KCJ11_MOUSE] This receptor is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. Can be blocked by extracellular barium. Can form cardiac and smooth muscle-type KATP channels with ABCC9. KCNJ11 forms the channel pore while ABCC9 is required for activation and regulation (By similarity).

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^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Ding D, Wang M, Wu JX, Kang Y, Chen L. The Structural Basis for the Binding of Repaglinide to the Pancreatic KATP Channel. Cell Rep. 2019 May 7;27(6):1848-1857.e4. doi: 10.1016/j.celrep.2019.04.050. PMID:31067468 doi:http://dx.doi.org/10.1016/j.celrep.2019.04.050

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/6jb1"

@@ Line 3: / Line 3: @@
 <StructureSection load='6jb1' size='340' side='right'caption='[[6jb1]], [[Resolution|resolution]] 3.30&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[6jb1]] is a 8 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6JB1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6JB1 FirstGlance]. <br>
+<table><tr><td colspan='2'>[[6jb1]] is a 8 chain structure with sequence from [http://en.wikipedia.org/wiki/Golden_hamster Golden hamster] and [http://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6JB1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6JB1 FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AGS:PHOSPHOTHIOPHOSPHORIC+ACID-ADENYLATE+ESTER'>AGS</scene>, <scene name='pdbligand=AJP:Digitonin'>AJP</scene>, <scene name='pdbligand=BJX:Repaglinide'>BJX</scene>, <scene name='pdbligand=POV:(2S)-3-(HEXADECANOYLOXY)-2-[(9Z)-OCTADEC-9-ENOYLOXY]PROPYL+2-(TRIMETHYLAMMONIO)ETHYL+PHOSPHATE'>POV</scene>, <scene name='pdbligand=PTY:PHOSPHATIDYLETHANOLAMINE'>PTY</scene></td></tr>
+<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Kcnj11 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 LK3 transgenic mice]), Abcc8 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10036 Golden hamster])</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=6jb1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6jb1 OCA], [http://pdbe.org/6jb1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6jb1 RCSB], [http://www.ebi.ac.uk/pdbsum/6jb1 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6jb1 ProSAT]</span></td></tr>
 </table>
@@ Line 22: / Line 23: @@
 __TOC__
 </StructureSection>
+[[Category: Golden hamster]]
 [[Category: Large Structures]]
+[[Category: Lk3 transgenic mice]]
 [[Category: Chen, L]]
 [[Category: Ding, D]]

6jb1

From Proteopedia

Revision as of 08:11, 6 November 2019

Structure of pancreatic ATP-sensitive potassium channel bound with repaglinide and ATPgammaS at 3.3A resolution

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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