Structure of PDB 4qoc Chain G

Receptor sequence

>4qocG (length=94) Species: 9606 (Homo sapiens) [Search protein sequence]

QIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLY
DEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVN

3D structure

PDB

4qoc Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction.

Chain

Resolution

1.7 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	35T	G	R97 K98	R80 K81	MOAD: ic50=0.12nM BindingDB: IC50=0.100000nM
BS02	35T	G	I61 Y67 V93 K94 H96 I99	I44 Y50 V76 K77 H79 I82	MOAD: ic50=0.12nM BindingDB: IC50=0.100000nM

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

View graph for
Cellular Component

External links

PDB	RCSB:4qoc, PDBe:4qoc, PDBj:4qoc
PDBsum	4qoc
PubMed	25042256
UniProt	Q00987\|MDM2_HUMAN E3 ubiquitin-protein ligase Mdm2 (Gene Name=MDM2)

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