Structure of PDB 4oas Chain A

Receptor sequence
>4oasA (length=93) Species: 9606 (Homo sapiens) [Search protein sequence]
QIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLY
DEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVV
3D structure
PDB4oas Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2-p53 Inhibitor in Clinical Development.
ChainA
Resolution1.7 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.3.2.27: RING-type E3 ubiquitin transferase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 2SW A L54 G58 Q59 I61 V93 K94 H96 I99 Y100 L37 G41 Q42 I44 V76 K77 H79 I82 Y83 MOAD: Kd=0.045nM
PDBbind-CN: -logKd/Ki=10.00,IC50=0.10nM
BindingDB: IC50=0.100000nM,Kd=0.036000nM
Gene Ontology
Biological Process
GO:0043066 negative regulation of apoptotic process
GO:0051726 regulation of cell cycle
Cellular Component
GO:0005634 nucleus

View graph for
Biological Process

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Cellular Component
External links
PDB RCSB:4oas, PDBe:4oas, PDBj:4oas
PDBsum4oas
PubMed24456472
UniProtQ00987|MDM2_HUMAN E3 ubiquitin-protein ligase Mdm2 (Gene Name=MDM2)

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