Structure of PDB 5h24 Chain A

Receptor sequence

>5h24A (length=364) Species: 9606 (Homo sapiens) [Search protein sequence]

KCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYEC
HSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIIN
PITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLV
AIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKE
SYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCEN
AIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKM
LALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSRDSSILI
AVCDDASIWRWDRL

3D structure

PDB

5h24 Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy

Chain

Resolution

2.5 Å

3D
structure

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Enzymatic activity

Enzyme Commision number

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	peptide	A	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	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
BS02	LQG	A	F97 Y148 N194 K211 L240 D310 Y365 R367	F21 Y72 N118 K135 L164 D234 Y289 R291	BindingDB: IC50=1000nM

External links

PDB	RCSB:5h24, PDBe:5h24, PDBj:5h24
PDBsum	5h24
PubMed	28092155
UniProt	O75530\|EED_HUMAN Polycomb protein EED (Gene Name=EED)

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