Structure of PDB 2wqb Chain A

Receptor sequence
>2wqbA (length=289) Species: 9606 (Homo sapiens) [Search protein sequence]
YPVLDWNDIKFQDVIGEGGQVLKARIKKDGLRMDAAIKRMKELEVLCKLG
HHPNIINLLGACEHRGYLYLAIEYAPHGNLLDFLRKSRVLETDPAFAIAN
STASTLSSQQLLHFAADVARGMDYLSQKQFIHRNLAARNILVGENYVAKI
ADFGLSRGQEVYVKKTGRLPVRWMAIESLNYSVYTTNSDVWSYGVLLWEI
VSLGGTPYCGMTCAELYEKLPQGYRLEKPLNCDDEVYDLMRQCWREKPYE
RPSFAQILVSLNRMLEERKTYVNTTLYEKFTYAGIDCSA
3D structure
PDB2wqb Novel Thienopyrimidine and Thiazolopyrimidine Kinase Inhibitors with Activity Against Tie-2 in Vitro and in Vivo.
ChainA
Resolution2.95 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) N964 A966 R968 N969 D982 Y992 R999
Catalytic site (residue number reindexed from 1) N134 A136 R138 N139 D152 Y162 R168
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 QQ1 A A853 K855 I902 E903 Y904 A905 N969 F983 A36 K38 I72 E73 Y74 A75 N139 F153 PDBbind-CN: -logKd/Ki=6.27,IC50=0.54uM
BindingDB: IC50=540nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:2wqb, PDBe:2wqb, PDBj:2wqb
PDBsum2wqb
PubMed19854647
UniProtQ02763|TIE2_HUMAN Angiopoietin-1 receptor (Gene Name=TEK)

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