› 3lbl

X-ray diffraction
1.6Å resolution

Structure of human MDM2 protein in complex with Mi-63-analog

Released:
DOI: 10.2210/pdb3lbl/pdb
PDB entry 3lbl coloured by chain, front view.
PDB entry 3lbl coloured by chain, side view.
PDB entry 3lbl coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structures of low molecular weight inhibitors bound to MDMX and MDM2 reveal new approaches for p53-MDMX/MDM2 antagonist drug discovery.
Popowicz GM, Czarna A, Wolf S, Wang K, Wang W, Dömling A, Holak TA
Cell Cycle 9 1104-11 (2010)
PMID: 20237429

Function and Biology Details

Reaction catalysed: 
S-ubiquitinyl-[E2 ubiquitin-conjugating enzyme]-L-cysteine + [acceptor protein]-L-lysine = [E2 ubiquitin-conjugating enzyme]-L-cysteine + N(6)-ubiquitinyl-[acceptor protein]-L-lysine
Biochemical function:
  • not assigned
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-169499 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
E3 ubiquitin-protein ligase Mdm2 Chains: A, C, E
Molecule details ›
Chains: A, C, E
Length: 95 amino acids
Theoretical weight: 11.14 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q00987 (Residues: 18-111; Coverage: 19%)
Gene name: MDM2
Sequence domains: SWIB/MDM2 domain
Structure domains: SWIB/MDM2 domain

Ligands and Environments

1 bound ligand:
Ligand MI6 3 x MI6
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X10SA
Spacegroup: C2221
Unit cell:
a: 56.94Å b: 97.35Å c: 106.63Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.193 0.191 0.236
Expression system: Escherichia coli

Quick links

Citations

32 review citations

MDM2, MDMX and p53 in oncogenesis and cancer therapy.
Wade et al. (2013)
31 more

27 mentions without citation

The structure-based design of Mdm2/Mdmx-p53 inhibitors gets serious.
Popowicz et al. (2011)
26 more