› 6rv3

X-ray diffraction
2.9Å resolution

Crystal structure of the human two pore domain potassium ion channel TASK-1 (K2P3.1) in a closed conformation with a bound inhibitor BAY 1000493

Released:
DOI: 10.2210/pdb6rv3/pdb
PDB entry 6rv3 coloured by chain, front view.
PDB entry 6rv3 coloured by chain, side view.
PDB entry 6rv3 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
A lower X-gate in TASK channels traps inhibitors within the vestibule.
Rödström KEJ, Kiper AK, Zhang W, Rinné S, Pike ACW, Goldstein M, Conrad LJ, Delbeck M, Hahn MG, Meier H, Platzk M, Quigley A, Speedman D, Shrestha L, Mukhopadhyay SMM, Burgess-Brown NA, Tucker SJ, Müller T, Decher N, Carpenter EP
Nature 582 443-447 (2020)
PMID: 32499642

Function and Biology Details

Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-518081 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Potassium channel subfamily K member 3 Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 264 amino acids
Theoretical weight: 30.12 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: O14649 (Residues: 1-259; Coverage: 66%)
Gene names: KCNK3, TASK, TASK1
Sequence domains: Ion channel

Ligands and Environments

5 bound ligands:
Ligand K 8 x K
Ligand Y01 7 x Y01
Ligand DMU 4 x DMU
Ligand PC1 3 x PC1
Ligand KKQ 2 x KKQ
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I24
Unit cell:
a: 45.07Å b: 204.5Å c: 239.32Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.235 0.235 0.242
Expression system: Spodoptera frugiperda

Quick links

Citations

6 review citations

Potassium Channels as a Target for Cancer Therapy: Current Perspectives.
Zúñiga et al. (2022)
5 more

7 mentions without citation

Structural Insights into the Mechanisms and Pharmacology of K2P Potassium Channels.
Natale et al. (2021)
6 more