› 3vp3

X-ray diffraction
2.7Å resolution

Crystal structure of human glutaminase in complex with inhibitor 3

Released:
DOI: 10.2210/pdb3vp3/pdb
PDB entry 3vp3 coloured by chain, front view.
PDB entry 3vp3 coloured by chain, side view.
PDB entry 3vp3 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism.
Thangavelu K, Pan CQ, Karlberg T, Balaji G, Uttamchandani M, Suresh V, Schüler H, Low BC, Sivaraman J
Proc Natl Acad Sci U S A 109 7705-10 (2012)
PMID: 22538822

Function and Biology Details

Reaction catalysed: 
L-glutamine + H(2)O = L-glutamate + NH(3)
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
homo tetramer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-131797 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Glutaminase kidney isoform, mitochondrial 65 kDa chain Chain: A
Molecule details ›
Chain: A
Length: 315 amino acids
Theoretical weight: 34.69 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: O94925 (Residues: 221-533; Coverage: 47%)
Gene names: GLS, GLS1, KIAA0838
Sequence domains: Glutaminase
Structure domains: DD-peptidase/beta-lactamase superfamily

Ligands and Environments

2 bound ligands:
Ligand BP8 1 x BP8
Ligand SO4 1 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSRRC BEAMLINE BL13B1
Spacegroup: I4122
Unit cell:
a: 139.825Å b: 139.825Å c: 158.043Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.195 0.195 0.215
Expression system: Escherichia coli

Quick links

Citations

28 review citations

Glutaminolysis as a target for cancer therapy.
Jin et al. (2016)
27 more

3 mentions without citation

A tale of two glutaminases: homologous enzymes with distinct roles in tumorigenesis.
Katt et al. (2017)
2 more