Crystallization (Comment) | Organism |
---|---|
structure of the mature form in complex with inhibitor harmine, to 1.9 A resolution. The phosphorylation of residue S350 increases the stability of DYRK3 and enhances its kinase activity. The N-terminal autophosphorylation accessory domain stabilizes the DYRK3 protein, followed by autophosphorylation of the tyrosine of the activation loop, which is important for kinase activity | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
K238M | loss of kinase activity | Homo sapiens |
S350A | 50% of wild-type activity, melting temperature decreases by almost 5 degrees compared to wild-type | Homo sapiens |
S350D | 80% of wild-type activity, melting temperature is similar to wild-type | Homo sapiens |
S350E | 90% of wild-type activity, melting temperature decreases by 2 degrees compared to wild-type | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
GSK-626616 | i.e. (5Z)-2-(2,6-dichloroanilino)-5-[(quinoxalin-6-yl)methylidene]-1,3-thiazol-4(5H)-one, ATP competitive inhibitor | Homo sapiens | |
harmine | ATP competitive inhibitor | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O43781 | - |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | residue S350 is a phosphorylation site | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + PRAS40 | i.e. proline rich Akt substrate 40 | Homo sapiens | ADP + phosphorylated PRAS40 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
dual specificity tyrosine-phosphorylation-regulated kinase 3 | - |
Homo sapiens |
DYRK3 | - |
Homo sapiens |
Temperature Stability Minimum [°C] | Temperature Stability Maximum [°C] | Comment | Organism |
---|---|---|---|
41.8 | - |
melting temperature, mutant S350A | Homo sapiens |
44.3 | - |
melting temperature, mutant S350E | Homo sapiens |
46.5 | - |
melting temperature, wild-type | Homo sapiens |
46.8 | - |
melting temperature, mutant S350D | Homo sapiens |