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Literature summary for 2.7.11.26 extracted from

  • Bao, C.; Bajrami, B.; Marcotte, D.J.; Chodaparambil, J.V.; Kerns, H.M.; Henderson, J.; Wei, R.; Gao, B.; Dillon, G.M.
    Mechanisms of regulation and diverse activities of tau-tubulin kinase (TTBK) isoforms (2021), Cell. Mol. Neurobiol., 41, 669-685 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
isoform TTBK1 is expressed in HEK-293T cells Mus musculus
isoform TTBK2 kinase domain is expressed in Escherichia coli strain NEB2523 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
isoform TTBK2 kinase domain with ADP, using 0.1 M Tris pH 8.5, 10% (v/v) glycerol and 2 M Na/K phosphate Mus musculus
isoform TTBK2 kinase domain with ADP, using 0.1 M Tris pH 8.5, 10% (v/v) glycerol and 2 M Na/K phosphate Homo sapiens

Protein Variants

Protein Variants Comment Organism
K50A kinase-dead mutant Homo sapiens
K63A kinase-dead mutant Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-(2-amino-5,6,7,8-tetrahydropyrimido[4',5':3,4]cyclohept[1,2-b]indol-11-yl)-2-methyl-3-butyn-2-ol
-
Homo sapiens
BIIB-TTBKi-284
-
Mus musculus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Mus musculus
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + tau-protein Mus musculus
-
ADP + O-phospho-tau-protein
-
?
ATP + tau-protein Homo sapiens
-
ADP + O-phospho-tau-protein
-
?
ATP + tau-protein Homo sapiens isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422 ADP + O-phospho-tau-protein
-
?
ATP + tau-protein Mus musculus isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422 ADP + O-phospho-tau-protein
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q5TCY1
-
-
Homo sapiens Q6IQ55
-
-
Mus musculus Q3UVR3
-
-
Mus musculus Q6PCN3
-
-

Purification (Commentary)

Purification (Comment) Organism
nickel resin column chromatography and Superdex 75 gel filtration Mus musculus
nickel resin column chromatography and Superdex 75 gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Homo sapiens
-
cartilage
-
Mus musculus
-
cerebellum
-
Mus musculus
-
cerebellum high expression Mus musculus
-
cerebral cortex
-
Mus musculus
-
cerebral cortex high expression Mus musculus
-
cerebral cortical neuron highest expression Mus musculus
-
additional information not detected in blood, sciatic nerve, small intestine, skin, pancreas, muscle, and cartilage Mus musculus
-
additional information not detected in blood, small intestine, spleen, skin, and pancreas Mus musculus
-
muscle weakest expression Mus musculus
-
sciatic nerve
-
Mus musculus
-
spinal cord high expression Mus musculus
-
spinal ganglion
-
Mus musculus
-
spleen weakest expression Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + HLSNVSSTGSIDMVDSPQLATLADEVSASLAK
-
Mus musculus ADP + HLSNVSSTGSIDMVDpSPQLATLADEVSASLAK
-
?
ATP + HLSNVSSTGSIDMVDSPQLATLADEVSASLAK
-
Homo sapiens ADP + HLSNVSSTGSIDMVDpSPQLATLADEVSASLAK
-
?
ATP + tau-protein
-
Mus musculus ADP + O-phospho-tau-protein
-
?
ATP + tau-protein
-
Homo sapiens ADP + O-phospho-tau-protein
-
?
ATP + tau-protein isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422 Homo sapiens ADP + O-phospho-tau-protein
-
?
ATP + tau-protein isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422 Mus musculus ADP + O-phospho-tau-protein
-
?
additional information isoform TTBK1 is autophosphorylated Homo sapiens ?
-
-
additional information isoform TTBK1 is autophosphorylated Mus musculus ?
-
-
additional information isoform TTBK2 is autophosphorylated Mus musculus ?
-
-
additional information isoform TTBK2 is autophosphorylated Homo sapiens ?
-
-

Synonyms

Synonyms Comment Organism
tau-tubulin kinase
-
Mus musculus
tau-tubulin kinase
-
Homo sapiens
TTBK1 isoform Homo sapiens
TTBK1 isoform Mus musculus
TTBK2 isoform Mus musculus
TTBK2 isoform Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000095
-
isoform TTBK1, pH and temperature not specified in the publication Mus musculus BIIB-TTBKi-284
0.000738
-
isoform TTBK1, pH and temperature not specified in the publication Homo sapiens 4-(2-amino-5,6,7,8-tetrahydropyrimido[4',5':3,4]cyclohept[1,2-b]indol-11-yl)-2-methyl-3-butyn-2-ol
0.000801
-
isoform TTBK1, pH and temperature not specified in the publication Homo sapiens 4-(2-amino-5,6,7,8-tetrahydropyrimido[4',5':3,4]cyclohept[1,2-b]indol-11-yl)-2-methyl-3-butyn-2-ol