Structure of PDB 2x2k Chain A

Receptor sequence
>2x2kA (length=290) Species: 9606 (Homo sapiens) [Search protein sequence]
GPLSLSVDAFKIPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGY
TTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLL
IVEYAKYGSLRGFLRESRKVRALTMGDLISFAWQISQGMQYLAEMKLVHR
DLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESL
FDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERP
DNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRR
3D structure
PDB2x2k Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors.
ChainA
Resolution2.6 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D850 D874 A876 R878 N879 D892
Catalytic site (residue number reindexed from 1) D127 D151 A153 R155 N156 D169
Enzyme Commision number 2.7.10.1: receptor protein-tyrosine 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 X2K A L730 V738 A756 Y806 A807 G810 L881 D892 L28 V36 A54 Y104 A105 G108 L158 D169 PDBbind-CN: -logKd/Ki=6.52,IC50=0.30uM
BindingDB: IC50=300nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine 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:2x2k, PDBe:2x2k, PDBj:2x2k
PDBsum2x2k
PubMed20117004
UniProtP07949|RET_HUMAN Proto-oncogene tyrosine-protein kinase receptor Ret (Gene Name=RET)

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