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Discovery of imidazoquinolines as a novel class of potent, selective and in vivo efficacious COT kinase inhibitors

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

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EC 2.7.11.25: Mitogen-activated protein kinase kinase kinase

Reaction catalysed:
ATP + a protein = ADP + a phosphoprotein
Systematic name:
ATP:protein phosphotransferase (MAPKKKK-activated)
Alternative Name(s):
  • CMos
  • CRaf
  • MAP kinase kinase kinase
  • MAP3K
  • MAPKKK
  • MEK kinase
  • MEKK
  • MEKK1
  • MEKK2
  • MEKK3
  • MLK-like mitogen-activated protein triple kinase
  • MLTK
  • MLTKa
  • MLTKb
  • Mil/Raf
  • REKS
  • STK28

GO terms

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

Sequence family

Pfam Protein family (Pfam)
PF00069
Domain description: Protein kinase domain
Occurring in:
  1. Mitogen-activated protein kinase kinase kinase 8
The deposited structure of PDB entry 5iu2 contains 2 copies of Pfam domain PF00069 (Protein kinase domain) in Mitogen-activated protein kinase kinase kinase 8. Showing 1 copy in chain B.

InterPro InterPro annotations
IPR000719
Domain description: Protein kinase domain
Occurring in:
  1. Mitogen-activated protein kinase kinase kinase 8
IPR008271
Domain description: Serine/threonine-protein kinase, active site
Occurring in:
  1. Mitogen-activated protein kinase kinase kinase 8
IPR011009
Domain description: Protein kinase-like domain superfamily
Occurring in:
  1. Mitogen-activated protein kinase kinase kinase 8

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. Mitogen-activated protein kinase kinase kinase 8
The deposited structure of PDB entry 5iu2 contains 2 copies of CATH domain 1.10.510.10 (Transferase(Phosphotransferase); domain 1) in Mitogen-activated protein kinase kinase kinase 8. Showing 1 copy in chain B.
3.30.200.20
Class: Alpha Beta
Architecture: 2-Layer Sandwich
Topology: Phosphorylase Kinase; domain 1
Homology: Phosphorylase Kinase; domain 1
Occurring in:
  1. Mitogen-activated protein kinase kinase kinase 8
The deposited structure of PDB entry 5iu2 contains 2 copies of CATH domain 3.30.200.20 (Phosphorylase Kinase; domain 1) in Mitogen-activated protein kinase kinase kinase 8. Showing 1 copy in chain B.

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