|Entry||Database: PDB / ID: 6jb3|
|Title||Structure of SUR1 subunit bound with repaglinide|
|Components||ATP-binding cassette sub-family C member 8 isoform X2|
|Keywords||MEMBRANE PROTEIN / KATP / channel / repaglinide / Kir / ABC transporter / SUR / diabetes / insulin secretagogue|
|Function / homology|
Function and homology information
sulfonylurea receptor activity / potassium ion transport / ATPase-coupled transmembrane transporter activity / ATPase activity / integral component of membrane / ATP binding / plasma membrane
AAA+ ATPase domain / ABC transporter integral membrane type-1 fused domain profile. / ABC transporter transmembrane region / ABC transporter / ABC transporter type 1, transmembrane domain superfamily / P-loop containing nucleoside triphosphate hydrolase / ABC transporter, conserved site / ABC transporter type 1, transmembrane domain / ABC transporter-like / ATP-binding cassette, ABC transporter-type domain profile. ...AAA+ ATPase domain / ABC transporter integral membrane type-1 fused domain profile. / ABC transporter transmembrane region / ABC transporter / ABC transporter type 1, transmembrane domain superfamily / P-loop containing nucleoside triphosphate hydrolase / ABC transporter, conserved site / ABC transporter type 1, transmembrane domain / ABC transporter-like / ATP-binding cassette, ABC transporter-type domain profile. / ATP-binding cassette subfamily C member 8 / Sulphonylurea receptor / ABC transporters family signature.
ATP-binding cassette sub-family C member 8 isoform X2
|Biological species||Mesocricetus auratus (golden hamster)|
|Method||ELECTRON MICROSCOPY / single particle reconstruction / cryo EM / Resolution: 3.53 Å|
|Authors||Chen, L. / Ding, D. / Wang, M. / Wu, J.-X. / Kang, Y.|
|Funding support|| China, 4items |
|Citation||Journal: Cell Rep / Year: 2019|
Title: The Structural Basis for the Binding of Repaglinide to the Pancreatic K Channel.
Authors: Dian Ding / Mengmeng Wang / Jing-Xiang Wu / Yunlu Kang / Lei Chen /
Abstract: 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 ...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 (K). However, the mechanisms by which RPG binds to the K channel are poorly understood. Here, we describe two cryo-EM structures: the pancreatic K channel in complex with inhibitory RPG and adenosine-5'-(γ-thio)-triphosphate (ATPγS) at 3.3 Å 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.
SummaryFull reportAbout validation report
|Structure viewer||Molecule: |
Downloads & links
B: ATP-binding cassette sub-family C member 8 isoform X2
|#1: Protein/peptide|| |
Mass: 177295.516 Da / Num. of mol.: 1
Source method: isolated from a genetically manipulated source
Source: (gene. exp.) Mesocricetus auratus (golden hamster) / Gene: Abcc8 / Production host: Homo sapiens (human) / References: UniProt: A0A1U7R319
|#2: Chemical|| ChemComp-BJX / |
|#3: Chemical|| ChemComp-AJP / |
|Experiment||Method: ELECTRON MICROSCOPY|
|EM experiment||Aggregation state: PARTICLE / 3D reconstruction method: single particle reconstruction|
|Component||Name: SUR1ABCC8 / Type: COMPLEX / Entity ID: 1 / Source: RECOMBINANT|
|Source (natural)||Organism: Mus musculus (house mouse)|
|Source (recombinant)||Organism: Homo sapiens (human)|
|Buffer solution||pH: 7.5|
|Specimen||Embedding applied: NO / Shadowing applied: NO / Staining applied: NO / Vitrification applied: YES|
|Vitrification||Cryogen name: ETHANE|
-Electron microscopy imaging
Model: Titan Krios / Image courtesy: FEI Company
|Microscopy||Model: FEI TITAN KRIOS|
|Electron gun||Electron source: FIELD EMISSION GUN / Accelerating voltage: 300 kV / Illumination mode: FLOOD BEAM|
|Electron lens||Mode: BRIGHT FIELDBright-field microscopy|
|Image recording||Electron dose: 50 e/Å2 / Film or detector model: GATAN K2 QUANTUM (4k x 4k)|
|Software||Name: PHENIX / Version: (1.12_2829: ???) / Classification: refinement|
|EM software||Name: RELION / Version: 2 / Category: 3D reconstruction|
|CTF correction||Type: NONE|
|3D reconstruction||Resolution: 3.53 Å / Resolution method: FSC 0.143 CUT-OFF / Num. of particles: 653991 / Symmetry type: POINT|
|Refinement||Resolution: 3.001→74.897 Å / SU ML: 1.4 / σ(F): 0.01 / Phase error: 64.36 / Stereochemistry target values: MLHL|
|Solvent computation||Shrinkage radii: 0.9 Å / VDW probe radii: 1.11 Å / Solvent model: FLAT BULK SOLVENT MODEL|
|Refine LS restraints|
Refinement-ID: ELECTRON MICROSCOPY
|LS refinement shell|
Refinement-ID: ELECTRON MICROSCOPY
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