› 4iu6

X-ray diffraction
1.9Å resolution

Human Methionine Aminopeptidase in complex with FZ1: Pyridinylquinazolines Selectively Inhibit Human Methionine Aminopeptidase-1

Released:
DOI: 10.2210/pdb4iu6/pdb
PDB entry 4iu6 coloured by chain, front view.
PDB entry 4iu6 coloured by chain, side view.
PDB entry 4iu6 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
Zhang F, Bhat S, Gabelli SB, Chen X, Miller MS, Nacev BA, Cheng YL, Meyers DJ, Tenney K, Shim JS, Crews P, Amzel LM, Ma D, Liu JO
J Med Chem 56 3996-4016 (2013)
PMID: 23634668

Function and Biology Details

Reaction catalysed: 
Release of N-terminal amino acids, preferentially methionine, from peptides and arylamides.
Biochemical function:
Biological process:
Cellular component:
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: 384 amino acids
Theoretical weight: 43 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P53582 (Residues: 1-384; Coverage: 100%)
Gene names: KIAA0094, METAP1
Sequence domains:
Structure domains: Creatinase/methionine aminopeptidase superfamily

Ligands and Environments

4 bound ligands:
Ligand CO 3 x CO
Ligand K 1 x K
Ligand FZ1 1 x FZ1
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: 47.303Å b: 77.344Å c: 47.821Å
α: 90° β: 91.49° γ: 90°
R-values:
R R work R free
0.175 0.172 0.223
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

1 review citation

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

6 mentions without citation

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