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Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency

Source organism: Homo sapiens
Biochemical function: ATP binding
Biological process: protein phosphorylation
Cellular component: not assigned

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EC 2.7.10.2: Non-specific protein-tyrosine kinase

Reaction catalysed:
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Systematic name:
ATP:[protein]-L-tyrosine O-phosphotransferase (non-specific)
Alternative Name(s):
  • ABL
  • ABL1
  • ABL2
  • ABLL
  • ACK1
  • ACK2
  • AGMX1
  • ARG
  • ATK
  • ATP:protein-tyrosine O-phosphotransferase
  • BLK
  • BMX
  • BRK
  • BTK
  • BTKL
  • Bmk
  • Bruton's tyrosine kinase
  • Bsk
  • CAKb
  • CHK
  • CSK
  • CTK
  • CYL
  • Cdgip
  • Cytoplasmic protein tyrosine kinase
  • EMT
  • ETK
  • FAK
  • FAK2
  • FER
  • FES
  • FGR
  • FPS
  • FRK
  • FYN
  • Fadk
  • Fert1/2
  • Focal adhesion kinase
  • HCK
  • HCTK
  • HYL
  • IMD1
  • ITK
  • IYK
  • JAK1
  • JAK2
  • JAK3
  • JTK1
  • JTK9
  • Janus kinase 1
  • Janus kinase 2
  • Janus kinase 3
  • L-JAK
  • LCK
  • LSK
  • LYN
  • MATK
  • Ntk
  • P60c-src protein tyrosine kinase
  • PKB
  • PSCTK
  • PSCTK1
  • PSCTK2
  • PSCTK4
  • PSCTK5
  • PTK2
  • PTK2B
  • PTK6
  • PYK2
  • Protein-tyrosine kinase
  • RAFTK
  • RAK
  • Rlk
  • SLK
  • SRC
  • SRC2
  • SRK
  • SRM
  • SRMS
  • STD
  • SYK
  • SYN
  • Sik
  • TEC
  • TNK1
  • TXK
  • TYK2
  • TYK3
  • Tck
  • Tsk
  • YES1
  • YK2
  • ZAP70

GO terms

Biochemical function:
Biological process:
Cellular component:
  • not assigned

Sequence family

Pfam Protein family (Pfam)
PF07714
Domain description: Protein tyrosine and serine/threonine kinase
Occurring in:
  1. Protein-tyrosine kinase 2-beta
The deposited structure of PDB entry 5tob contains 1 copy of Pfam domain PF07714 (Protein tyrosine and serine/threonine kinase) in Protein-tyrosine kinase 2-beta. Showing 1 copy in chain A.

InterPro InterPro annotations
IPR001245
Domain description: Serine-threonine/tyrosine-protein kinase, catalytic domain
Occurring in:
  1. Protein-tyrosine kinase 2-beta
IPR008266
Domain description: Tyrosine-protein kinase, active site
Occurring in:
  1. Protein-tyrosine kinase 2-beta
IPR017441
Domain description: Protein kinase, ATP binding site
Occurring in:
  1. Protein-tyrosine kinase 2-beta
IPR020635
Domain description: Tyrosine-protein kinase, catalytic domain
Occurring in:
  1. Protein-tyrosine kinase 2-beta
IPR000719
Domain description: Protein kinase domain
Occurring in:
  1. Protein-tyrosine kinase 2-beta
IPR011009
Domain description: Protein kinase-like domain superfamily
Occurring in:
  1. Protein-tyrosine kinase 2-beta

Structure domains

CATH CATH domains
1.10.510.10
Class: Mainly Alpha
Architecture: Orthogonal Bundle
Topology: Transferase(Phosphotransferase); domain 1
Homology: Transferase(Phosphotransferase) domain 1
Occurring in:
  1. Protein-tyrosine kinase 2-beta
The deposited structure of PDB entry 5tob contains 1 copy of CATH domain 1.10.510.10 (Transferase(Phosphotransferase); domain 1) in Protein-tyrosine kinase 2-beta. Showing 1 copy in chain A.
3.30.200.20
Class: Alpha Beta
Architecture: 2-Layer Sandwich
Topology: Phosphorylase Kinase; domain 1
Homology: Phosphorylase Kinase; domain 1
Occurring in:
  1. Protein-tyrosine kinase 2-beta
The deposited structure of PDB entry 5tob contains 1 copy of CATH domain 3.30.200.20 (Phosphorylase Kinase; domain 1) in Protein-tyrosine kinase 2-beta. Showing 1 copy in chain A.

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