Structure of PDB 4rx7 Chain A

Receptor sequence
>4rx7A (length=272) Species: 9606 (Homo sapiens) [Search protein sequence]
VYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILKNEPALKD
ELLAEANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRH
VTDKNIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGL
SKALRADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEA
FSYGQKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVEN
RPGFAAVELRLRNYYYDVVNHH
3D structure
PDB4rx7 Discovery and profiling of a selective and efficacious syk inhibitor.
ChainA
Resolution1.8 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D494 A496 R498 N499 D512 K533
Catalytic site (residue number reindexed from 1) D129 A131 R133 N134 D147 K168
Enzyme Commision number 2.7.10.2: non-specific 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 3YV A L377 A400 M448 E449 A451 G454 P455 R498 L501 D512 L15 A38 M83 E84 A86 G89 P90 R133 L136 D147 MOAD: ic50=5nM
PDBbind-CN: -logKd/Ki=8.30,IC50=5nM
BindingDB: IC50=104nM
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

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:4rx7, PDBe:4rx7, PDBj:4rx7
PDBsum4rx7
PubMed25633741
UniProtP43405|KSYK_HUMAN Tyrosine-protein kinase SYK (Gene Name=SYK)

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