Structure of PDB 5to8 Chain A

Receptor sequence
>5to8A (length=250) Species: 9606 (Homo sapiens) [Search protein sequence]
IAREDVVLNRILGEGFFGEVYEGVYTNHKGEKINVAVKTCKKDCTNKEKF
MSEAVIMKNLDHPHIVKLIGIIEPTWIIMELYPYGELGHYLERNKNSLKV
LTLVLYSLQICKAMAYLESCVHRDIAVRNILVASPECVKLGDFGLSRIKW
MSPESINFRRFTTASDVWMFAVCMWEILSFGKQPFFWLENKDVIGVLEKG
DRLPKPDLCPPVLYTLMTRCWDYDPSDRPRFTELVCSLSDVYQMEKDIAM
3D structure
PDB5to8 Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.
ChainA
Resolution1.9849 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D549 A551 R553 N554 D567
Catalytic site (residue number reindexed from 1) D124 A126 R128 N129 D142
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 7FM A L431 G432 E433 M502 E503 L504 Y505 G508 E509 R553 L556 L12 G13 E14 M79 E80 L81 Y82 G85 E86 R128 L131 MOAD: ic50=3.1nM
PDBbind-CN: -logKd/Ki=8.51,IC50=3.1nM
BindingDB: IC50=3.1nM
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:5to8, PDBe:5to8, PDBj:5to8
PDBsum5to8
PubMed27876318
UniProtQ14289|FAK2_HUMAN Protein-tyrosine kinase 2-beta (Gene Name=PTK2B)

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