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Literature summary for 2.7.11.26 extracted from

  • Nozal, V.; Martinez, A.
    Tau tubulin kinase 1 (TTBK1), a new player in the fight against neurodegenerative diseases (2019), Eur. J. Med. Chem., 161, 39-47 .
    View publication on PubMed

Application

Application Comment Organism
medicine isoform TTBK1 is a target for the treatment of neurodegenerative diseases Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-bromo-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)benzoate
-
Homo sapiens
3-((5-((4-amino-4-methylcyclohexyl)amino)-pyrrolo[2,1-f][1,2,4] triazin-4-yl)amino)-5-bromophenol
-
Homo sapiens
3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + alpha-actin Homo sapiens
-
ADP + p35
-
?
ATP + mu-calpain Homo sapiens
-
ADP + calpastatin
-
?
ATP + tau-protein Homo sapiens isoform TTBK1 phosphorylates tau-protein at Ser198, Ser199, Ser202 and Ser422 ADP + O-phospho-tau-protein
-
?
ATP + TDP-43 Homo sapiens
-
ADP + phosphorylated TDP-43
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q5TCY1
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Homo sapiens
-
neuron
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + alpha-actin
-
Homo sapiens ADP + p35
-
?
ATP + mu-calpain
-
Homo sapiens ADP + calpastatin
-
?
ATP + tau-protein isoform TTBK1 phosphorylates tau-protein at Ser198, Ser199, Ser202 and Ser422 Homo sapiens ADP + O-phospho-tau-protein
-
?
ATP + TDP-43
-
Homo sapiens ADP + phosphorylated TDP-43
-
?

Subunits

Subunits Comment Organism
? x * 230000, SDS-PAGE Homo sapiens
? x * 142700, calculated from amino acid sequence Homo sapiens

Synonyms

Synonyms Comment Organism
Tau tubulin kinase 1
-
Homo sapiens
TTBK1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00012
-
isoform TTBK1, pH and temperature not specified in the publication Homo sapiens 3-((5-((4-amino-4-methylcyclohexyl)amino)-pyrrolo[2,1-f][1,2,4] triazin-4-yl)amino)-5-bromophenol

Expression

Organism Comment Expression
Homo sapiens isoform TTBK1 is upregulated in the frontal cortex of patients with Alzheimer's disease up