Structure of PDB 5iu2 Chain B

Receptor sequence
>5iu2B (length=313) Species: 9606 (Homo sapiens) [Search protein sequence]
LSSVRYGTVEDLLAFANHISNHFYGQRPQESGILLNMVITPQNGRYQIDS
DVLLIPWKLTYRNGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKP
SDVEIQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMR
EFEIIWVTKHVLKGLDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQ
MTEDVYFPKDLRGTEIYMSPEVILCRGHSTKADIYSLGATLIHMQTGTPP
WVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPGMRELIEASLERNPNHR
PRAADLLKHEALN
3D structure
PDB5iu2 Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors.
ChainB
Resolution2.7 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D253 K255 N258 D270 T290
Catalytic site (residue number reindexed from 1) D177 K179 N182 D194 T214
Enzyme Commision number 2.7.11.25: mitogen-activated protein kinase kinase kinase.
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 6DA B W132 L134 G150 V152 A165 K167 M207 A209 G210 G213 E217 S257 V260 V269 D270 W57 L59 G74 V76 A89 K91 M131 A133 G134 G137 E141 S181 V184 V193 D194 BindingDB: IC50=16nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

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Molecular Function
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Biological Process
External links
PDB RCSB:5iu2, PDBe:5iu2, PDBj:5iu2
PDBsum5iu2
PubMed27502541
UniProtP41279|M3K8_HUMAN Mitogen-activated protein kinase kinase kinase 8 (Gene Name=MAP3K8)

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