› 1dls

X-ray diffraction
2.3Å resolution

METHOTREXATE-RESISTANT VARIANTS OF HUMAN DIHYDROFOLATE REDUCTASE WITH SUBSTITUTION OF LEUCINE 22: KINETICS, CRYSTALLOGRAPHY AND POTENTIAL AS SELECTABLE MARKERS

Released:
DOI: 10.2210/pdb1dls/pdb
PDB entry 1dls coloured by chain, front view.
PDB entry 1dls coloured by chain, side view.
PDB entry 1dls coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Methotrexate-resistant variants of human dihydrofolate reductase with substitutions of leucine 22. Kinetics, crystallography, and potential as selectable markers.
Lewis WS, Cody V, Galitsky N, Luft JR, Pangborn W, Chunduru SK, Spencer HT, Appleman JR, Blakley RL
J Biol Chem 270 5057-64 (1995)
PMID: 7890613

Function and Biology Details

Reaction catalysed: 
5,6,7,8-tetrahydrofolate + NADP(+) = 7,8-dihydrofolate + NADPH
Biochemical function:
Biological process:
Cellular component:
Sequence domains:
Structure domain:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-132447 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Dihydrofolate reductase Chain: A
Molecule details ›
Chain: A
Length: 186 amino acids
Theoretical weight: 21.4 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: P00374 (Residues: 2-187; Coverage: 100%)
Gene name: DHFR
Sequence domains: Dihydrofolate reductase
Structure domains: Dihydrofolate Reductase, subunit A

Ligands and Environments


Cofactor: Ligand NDP 1 x NDP
1 bound ligand:
Ligand MTX 1 x MTX
No modified residues

Experiments and Validation Details

Entry percentile scores
Spacegroup: R3
Unit cell:
a: 87.496Å b: 87.496Å c: 76.733Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.156 not available not available
Expression system: Not provided

Quick links

Citations

12 review citations

Reactive nitrogen species in the chemical biology of inflammation.
Dedon et al. (2004)
11 more

21 mentions without citation

DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents.
Raimondi et al. (2019)
20 more