Structure of PDB 2zm3 Chain A

Receptor sequence
>2zm3A (length=303) Species: 9606 (Homo sapiens) [Search protein sequence]
SFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETR
VAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIM
ELMTRGDLKSYLRSLRPENPVLAPPSLSKMIQMAGEIADGMAYLNANKFV
HRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPE
SLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLD
KPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYS
EEN
3D structure
PDB2zm3 Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment
ChainA
Resolution2.5 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1135 R1139 N1140 D1153 E1162
Catalytic site (residue number reindexed from 1) D153 R157 N158 D171 E180
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 575 A L1005 Q1007 V1013 A1031 M1079 L1081 M1082 T1083 G1085 M1142 L26 Q28 V34 A52 M100 L102 M103 T104 G106 M160 MOAD: Kd=0.614uM
PDBbind-CN: -logKd/Ki=6.21,Kd=0.614uM
BindingDB: IC50=2420nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0004714 transmembrane receptor protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway
Cellular Component
GO:0016020 membrane

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Molecular Function

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Biological Process

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Cellular Component
External links
PDB RCSB:2zm3, PDBe:2zm3, PDBj:2zm3
PDBsum2zm3
PubMed18501599
UniProtP08069|IGF1R_HUMAN Insulin-like growth factor 1 receptor (Gene Name=IGF1R)

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