› 4o1d

X-ray diffraction
1.7Å resolution

Structural Basis for Resistance to Diverse Classes of NAMPT Inhibitors

Released:
DOI: 10.2210/pdb4o1d/pdb
PDB entry 4o1d coloured by chain, front view.
PDB entry 4o1d coloured by chain, side view.
PDB entry 4o1d coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural basis for resistance to diverse classes of NAMPT inhibitors.
Wang W, Elkins K, Oh A, Ho YC, Wu J, Li H, Xiao Y, Kwong M, Coons M, Brillantes B, Cheng E, Crocker L, Dragovich PS, Sampath D, Zheng X, Bair KW, O'Brien T, Belmont LD
PLoS One 9 e109366 (2014)
PMID: 25285661

Function and Biology Details

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

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-155082 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Nicotinamide phosphoribosyltransferase Chains: A, B
Molecule details ›
Chains: A, B
Length: 501 amino acids
Theoretical weight: 56.96 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P43490 (Residues: 1-491; Coverage: 100%)
Gene names: NAMPT, PBEF, PBEF1
Sequence domains:
Structure domains: Aldolase class I

Ligands and Environments

3 bound ligands:
Ligand DGB 2 x DGB
Ligand PO4 4 x PO4
Ligand EDO 15 x EDO
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.2
Spacegroup: P21
Unit cell:
a: 60.658Å b: 106.599Å c: 83.376Å
α: 90° β: 96.42° γ: 90°
R-values:
R R work R free
0.173 0.171 0.208
Expression system: Escherichia coli

Quick links

Citations

5 review citations

NAD+ salvage pathway in cancer metabolism and therapy.
Kennedy et al. (2016)
4 more

1 mention without citation

Structural basis for resistance to diverse classes of NAMPT inhibitors.
Wang et al. (2014)