Structure of PDB 5h24 Chain A Binding Site BS01

Receptor Information
>5h24 Chain A (length=364) Species: 9606 (Homo sapiens) [Search protein sequence] [Download receptor structure] [Download structure with residue number starting from 1] [View receptor structure]
KCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYEC
HSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIIN
PITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLV
AIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKE
SYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCEN
AIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKM
LALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSRDSSILI
AVCDDASIWRWDRL
Ligand information
>5h24 Chain C (length=29) Species: 9606 (Homo sapiens) [Search peptide sequence] [Download ligand structure] [Download structure with residue number starting from 1] [View ligand structure]
SMFSSNRQKILERTEILNQEWKQRRIQPV
Receptor-Ligand Complex Structure
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PDB5h24 Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
Resolution2.5 Å
Binding residue
(original residue number in PDB)
W103 H104 S105 K106 E107 D109 V112 Y154 S159 H160 P161 P177 I178 R201 L246 L247 L315 G316 D317 L318 K332 M336 F372 W373 Q374 L391 E392 E394 R420
Binding residue
(residue number reindexed from 1)
W27 H28 S29 K30 E31 D33 V36 Y78 S83 H84 P85 P101 I102 R125 L170 L171 L239 G240 D241 L242 K256 M260 F296 W297 Q298 L315 E316 E318 R344
Enzymatic activity
Enzyme Commision number ?
External links
PDB RCSB:5h24, PDBe:5h24, PDBj:5h24
PDBsum5h24
PubMed28092155
UniProtO75530|EED_HUMAN Polycomb protein EED (Gene Name=EED)

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