› 5eqg

X-ray diffraction
2.9Å resolution

Human GLUT1 in complex with inhibitor (2~{S})-3-(4-fluorophenyl)-2-[2-(3-hydroxyphenyl)ethanoylamino]-~{N}-[(1~{S})-1-phenylethyl]propanamide

Released:
DOI: 10.2210/pdb5eqg/pdb
PDB entry 5eqg coloured by chain, front view.
PDB entry 5eqg coloured by chain, side view.
PDB entry 5eqg coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Mechanism of inhibition of human glucose transporter GLUT1 is conserved between cytochalasin B and phenylalanine amides.
Kapoor K, Finer-Moore JS, Pedersen BP, Caboni L, Waight A, Hillig RC, Bringmann P, Heisler I, Müller T, Siebeneicher H, Stroud RM
Proc Natl Acad Sci U S A 113 4711-6 (2016)
PMID: 27078104

Function and Biology Details

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

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-145688 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Solute carrier family 2, facilitated glucose transporter member 1 Chain: A
Molecule details ›
Chain: A
Length: 492 amino acids
Theoretical weight: 54.13 KDa
Source organism: Homo sapiens
Expression system: Saccharomyces cerevisiae
UniProt:
  • Canonical: P11166 (Residues: 1-492; Coverage: 100%)
Gene names: GLUT1, SLC2A1
Sequence domains: Sugar (and other) transporter
Structure domains: MFS general substrate transporter like domains

Ligands and Environments

1 bound ligand:
Ligand 5RE 1 x 5RE
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 8.3.1
Spacegroup: C2
Unit cell:
a: 121.338Å b: 102.497Å c: 68.162Å
α: 90° β: 99.55° γ: 90°
R-values:
R R work R free
0.238 0.235 0.281
Expression system: Saccharomyces cerevisiae

Quick links

Citations

30 review citations

Glucose transporters in cancer - from tumor cells to the tumor microenvironment.
Ancey et al. (2018)
29 more

22 mentions without citation

Highlighting membrane protein structure and function: A celebration of the Protein Data Bank.
Li et al. (2021)
21 more