Structure of PDB 5tob Chain A

Receptor sequence
>5tobA (length=245) Species: 9606 (Homo sapiens) [Search protein sequence]
IAREDVVLNRILGEGFFGEVYEGVYTHKGEKINVAVKTCKDNKEKFMSEA
VIMKNLDHPHIVKLIGIIEPTWIIMELYPYGELGHYLERNKNSLKVLTLV
LYSLQICKAMAYLESINCVHRDIAVRNILVASPECVKLGDFGPIKWMSPE
SINFRRFTTASDVWMFAVCMWEILSFGKQPFFWLENKDVIGVLEKGDRLP
KPDLCPPVLYTLMTRCWDYDPSDRPRFTELVCSLSDVYQMEKDIA
3D structure
PDB5tob Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.
ChainA
Resolution2.117 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) D122 A124 R126 N127 D140
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 YAM A L431 G432 E433 M502 E503 L504 Y505 G508 E509 R553 L556 L12 G13 E14 M75 E76 L77 Y78 G81 E82 R126 L129 MOAD: ic50=13nM
PDBbind-CN: -logKd/Ki=8.82,IC50=1.5nM
BindingDB: IC50=13nM
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:5tob, PDBe:5tob, PDBj:5tob
PDBsum5tob
PubMed27876318
UniProtQ14289|FAK2_HUMAN Protein-tyrosine kinase 2-beta (Gene Name=PTK2B)

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