› 3gep

X-ray diffraction
2.6Å resolution

Human hypoxanthine guanine phosphoribosyltranserfase in complex with (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine

Released:
DOI: 10.2210/pdb3gep/pdb
PDB entry 3gep coloured by chain, front view.
PDB entry 3gep coloured by chain, side view.
PDB entry 3gep coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Inhibition of hypoxanthine-guanine phosphoribosyltransferase by acyclic nucleoside phosphonates: a new class of antimalarial therapeutics.
Keough DT, Hocková D, Holý A, Naesens LM, Skinner-Adams TS, Jersey Jd, Guddat LW
J Med Chem 52 4391-9 (2009)
PMID: 19527031

Function and Biology Details

Reaction catalysed: 
IMP + diphosphate = hypoxanthine + 5-phospho-alpha-D-ribose 1-diphosphate
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
homo tetramer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-132564 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Hypoxanthine-guanine phosphoribosyltransferase Chains: A, B
Molecule details ›
Chains: A, B
Length: 217 amino acids
Theoretical weight: 24.48 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P00492 (Residues: 2-218; Coverage: 100%)
Gene names: HPRT, HPRT1
Sequence domains: Phosphoribosyl transferase domain
Structure domains: Rossmann fold

Ligands and Environments

1 bound ligand:
Ligand 24H 2 x 24H
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU FR-E SUPERBRIGHT
Spacegroup: P21212
Unit cell:
a: 111.122Å b: 72.59Å c: 51.282Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.25 0.247 0.298
Expression system: Escherichia coli

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Citations

8 review citations

Purine and pyrimidine pathways as targets in Plasmodium falciparum.
Cassera et al. (2011)
7 more

1 mention without citation

From Exosome Biogenesis to Absorption: Key Takeaways for Cancer Research.
Lau et al. (2023)