› 8eio

Electron Microscopy
2.8Å resolution

The complex of phosphorylated human delta F508 cystic fibrosis transmembrane conductance regulator (CFTR) with elexacaftor (VX-445), lumacaftor (VX-809) and ATP/Mg

Released:
DOI: 10.2210/pdb8eio/pdb
PDB entry 8eio coloured by chain, front view.
PDB entry 8eio coloured by chain, side view.
PDB entry 8eio coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Molecular structures reveal synergistic rescue of Δ508 CFTR by Trikafta modulators.
Fiedorczuk K, Chen J
OpenAccess logo Science 378 284-290 (2022)
PMID: 36264792
Related structures: EMD-28160

Function and Biology Details

Reaction catalysed: 
ATP + H(2)O + closed Cl(-) channel = ADP + phosphate + open Cl(-) channel
Biochemical function:
  • not assigned
Biological process:
  • not assigned
Cellular component:
  • not assigned

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-273204 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Cystic fibrosis transmembrane conductance regulator Chain: A
Molecule details ›
Chain: A
Length: 1479 amino acids
Theoretical weight: 168.19 KDa
Source organism: Homo sapiens
Expression system: Homo sapiens
Cystic fibrosis transmembrane conductance regulator Chain: B
Molecule details ›
Chain: B
Length: 17 amino acids
Theoretical weight: 1.46 KDa
Source organism: Homo sapiens
Expression system: Homo sapiens

Ligands and Environments

6 bound ligands:
Ligand MG 2 x MG
Ligand ATP 2 x ATP
Ligand CLR 1 x CLR
Ligand D12 1 x D12
Ligand VX8 1 x VX8
Ligand WJX 1 x WJX
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 2.8Å
Relevant EMDB volumes: EMD-28160
Expression system: Homo sapiens

Quick links

Citations

11 review citations

Human disease models in drug development.
Loewa et al. (2023)
10 more

2 mentions without citation

Organic Synthesis and Current Understanding of the Mechanisms of CFTR Modulator Drugs Ivacaftor, Tezacaftor, and Elexacaftor.
Ferreira et al. (2024)
1 more