Structure of PDB 4zyi Chain A

Receptor sequence
>4zyiA (length=90) Species: 9606 (Homo sapiens) [Search protein sequence]
PASEQETLVRPKPLLLKLLKSVGQKDTYTMKEVLFYLGQYIMTKRLYDEK
QQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVV
3D structure
PDB4zyi Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
ChainA
Resolution1.67 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 4TH A Q24 L54 F55 G58 M62 Y67 Q72 F86 H96 I99 Q5 L34 F35 G38 M42 Y47 Q52 F66 H76 I79 MOAD: ic50=0.008uM
PDBbind-CN: -logKd/Ki=8.10,IC50=0.008uM
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:4zyi, PDBe:4zyi, PDBj:4zyi
PDBsum4zyi
PubMed26181851
UniProtQ00987|MDM2_HUMAN E3 ubiquitin-protein ligase Mdm2 (Gene Name=MDM2)

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