› 4hxx

X-ray diffraction
2.09Å resolution

Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1

Released:
DOI: 10.2210/pdb4hxx/pdb
PDB entry 4hxx coloured by chain, front view.
PDB entry 4hxx coloured by chain, side view.
PDB entry 4hxx coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1.
Zhang P, Yang X, Zhang F, Gabelli SB, Wang R, Zhang Y, Bhat S, Chen X, Furlani M, Amzel LM, Liu JO, Ma D
Bioorg Med Chem 21 2600-17 (2013)
PMID: 23507151

Function and Biology Details

Reaction catalysed: 
Release of N-terminal amino acids, preferentially methionine, from peptides and arylamides.
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-156814 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Methionine aminopeptidase 1 Chain: A
Molecule details ›
Chain: A
Length: 304 amino acids
Theoretical weight: 34.18 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P53582 (Residues: 81-384; Coverage: 79%)
Gene names: KIAA0094, METAP1
Sequence domains: Metallopeptidase family M24
Structure domains: Creatinase/methionine aminopeptidase superfamily

Ligands and Environments

4 bound ligands:
Ligand CO 3 x CO
Ligand K 1 x K
Ligand 1AY 1 x 1AY
Ligand SO4 2 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU FR-E+ DW
Spacegroup: P21
Unit cell:
a: 47.5Å b: 77.403Å c: 48.068Å
α: 90° β: 90.92° γ: 90°
R-values:
R R work R free
0.194 0.19 0.258
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

2 review citations

The Bengamides: A Mini-Review of Natural Sources, Analogues, Biological Properties, Biosynthetic Origins, and Future Prospects.
White et al. (2017)
1 more

4 mentions without citation

Advances in Bacterial Methionine Aminopeptidase Inhibition.
Helgren et al. (2016)
3 more