› 8bht

Electron Microscopy
3.1Å resolution

ABCG2 turnover-1 state with tariquidar bound

Released:
DOI: 10.2210/pdb8bht/pdb
PDB entry 8bht coloured by chain, front view.
PDB entry 8bht coloured by chain, side view.
PDB entry 8bht coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Differential dynamics and direct interaction of bound ligands with lipids in multidrug transporter ABCG2.
Rasouli A, Yu Q, Dehghani-Ghahnaviyeh S, Wen PC, Kowal J, Locher KP, Tajkhorshid E
OpenAccess logo Proc Natl Acad Sci U S A 120 e2213437120 (2023)
PMID: 36580587
Related structures: EMD-16069

Function and Biology Details

Reaction catalysed: 
ATP + H(2)O + xenobiotic(Side 1) = ADP + phosphate + xenobiotic(Side 2)
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-194005 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Broad substrate specificity ATP-binding cassette transporter ABCG2 Chains: A, B
Molecule details ›
Chains: A, B
Length: 665 amino acids
Theoretical weight: 73.53 KDa
Source organism: Homo sapiens
Expression system: Homo sapiens
UniProt:
  • Canonical: Q9UNQ0 (Residues: 2-655; Coverage: 100%)
Gene names: ABCG2, ABCP, BCRP, BCRP1, MXR
Sequence domains:

Ligands and Environments

3 bound ligands:
Ligand ATP 2 x ATP
Ligand CLR 2 x CLR
Ligand R1H 1 x R1H
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 3.1Å
Relevant EMDB volumes: EMD-16069
Expression system: Homo sapiens

Quick links

Citations

4 citation in other articles

Furmonertinib, a Third-Generation EGFR Tyrosine Kinase Inhibitor, Overcomes Multidrug Resistance through Inhibiting ABCB1 and ABCG2 in Cancer Cells.
Wu et al. (2023)
3 more

2 mentions without citation

How Cryo-EM Has Expanded Our Understanding of Membrane Transporters.
Baril et al. (2023)
1 more