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Literature summary for 2.7.11.26 extracted from
- Preferential selectivity of inhibitors with human tau protein kinase gsk3beta elucidates their potential roles for off-target Alzheimers therapy (2013), Int. J. Alzheimers Dis., 2013, 809386.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| AMP | AMP binding induces a conformational change in the ? -subunit activation loop of the kinase that allows phosphorylation of the activating residue Thr172 by AMPK upstream kinases | Homo sapiens |  |
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | tau kinase are drug target candidates for small molecule inhibitors | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| phylogenetic tree | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (4-amino-2-((4-chlorophenyl)amino)thiazol-5-yl)(3-nitrophenyl)methanone | enzyme binding structure analysis | Homo sapiens | |
| 3-[1H-indol-3-yl]-4-[2-[4-methylpiperazin-1-yl]quinazolin-4-yl]-1H-pyrrole-2,5-dione | enzyme binding structure analysis | Homo sapiens | |
| 4-[1-cyclohexyl-4-[4-fluorophenyl]-1H-imidazol-5-yl]pyrimidin-2-amine | enzyme binding structure analysis | Homo sapiens | |
| 5-[2-phenylpyrazolo[1,5-a]pyridin-3-yl]-1h-pyrazolo[3,4-c]pyridazin-3-amine | enzyme binding structure analysis | Homo sapiens | |
| 7-methoxy-1-methyl-9h-betacarboline | enzyme binding structure analysis | Homo sapiens | |
| additional information | inhibitor development using seven different scaffolds, scaffold 3-aminopyrrolidine exhibits high preferential affinity with GSK3beta. Interaction analysis of inhibitor scaffolds with different protein kinases, overview | Homo sapiens | |
| N-[3-cyano-6-[3-[1-piperidinyl]propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]1-naphthalenecarboxamide | enzyme binding structure analysis | Homo sapiens | |
| [3R]-1-[5-methyl-7Hpyrrolo[2,3-d]pyrimidin-4-yl]pyrrolidin-3-amine | enzyme binding structure analysis | Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [tau-protein] | Homo sapiens | - |
ADP + O-phospho-[tau-protein] | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P49841 | - |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| phosphoprotein | AMP binding induces a conformational change in the ? -subunit activation loop of the kinase that allows phosphorylation of the activating residue Thr172 by AMPK upstream kinases | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [tau-protein] | - |
Homo sapiens | ADP + O-phospho-[tau-protein] | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| dimer | GSK3beta enzyme is composed of three domains: an N-terminal domain consisting of a closed beta-barrel structure, a C-terminal domain containing a kinase fold structure, and a small extradomain subsequent to the C-terminal domain. The catalytic site is between the two major domains and has an ATP analogue molecule in its ATP binding site | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| GSK3B | - |
Homo sapiens |
| GSK3beta | - |
Homo sapiens |
| tau protein kinase | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000021 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-[1H-indol-3-yl]-4-[2-[4-methylpiperazin-1-yl]quinazolin-4-yl]-1H-pyrrole-2,5-dione | |
| 0.00013 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-[1-cyclohexyl-4-[4-fluorophenyl]-1H-imidazol-5-yl]pyrimidin-2-amine | |
| 0.00035 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-methoxy-1-methyl-9h-betacarboline | |
| 0.0019 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-[2-phenylpyrazolo[1,5-a]pyridin-3-yl]-1h-pyrazolo[3,4-c]pyridazin-3-amine | |
| 0.002 | - |
pH and temperature not specified in the publication | Homo sapiens | (4-amino-2-((4-chlorophenyl)amino)thiazol-5-yl)(3-nitrophenyl)methanone | |
| 0.0032 | - |
pH and temperature not specified in the publication | Homo sapiens | [3R]-1-[5-methyl-7Hpyrrolo[2,3-d]pyrimidin-4-yl]pyrrolidin-3-amine | |
| 0.0032 | - |
pH and temperature not specified in the publication | Homo sapiens | N-[3-cyano-6-[3-[1-piperidinyl]propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]1-naphthalenecarboxamide | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| evolution | sequence comparisons of diverse protein kinases, phylogenetic tree of tau protein kinases and analysis | Homo sapiens |
| malfunction | the abnormal phosphorylation of tau leads to the formation of neurofibrillary tangles produced by the action of tau kinases, resulting in the loss of neurons and synapse, leading to dementia | Homo sapiens |
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