Structure of PDB 5hmi Chain B

Receptor sequence
>5hmiB (length=100) Species: 9606 (Homo sapiens) [Search protein sequence]
PASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLYYLGQYIMTKRLYDE
KQQHIVHCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSAGA
3D structure
PDB5hmi Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
ChainB
Resolution1.74 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 62T B K51 Y55 K32 Y36 MOAD: ic50=0.015uM
BS02 62T B L54 G58 I61 M62 Y67 Q72 F91 V93 H96 I99 Y100 L35 G39 I42 M43 Y48 Q53 F72 V74 H77 I80 Y81 MOAD: ic50=0.015uM
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:5hmi, PDBe:5hmi, PDBj:5hmi
PDBsum5hmi
PubMed26985323
UniProtQ00987|MDM2_HUMAN E3 ubiquitin-protein ligase Mdm2 (Gene Name=MDM2)

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