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Literature summary for 2.7.12.1 extracted from

  • Kim, K.; Cha, J.S.; Cho, Y.S.; Kim, H.; Chang, N.; Kim, H.J.; Cho, H.S.
    Crystal structure of human dual-specificity tyrosine-regulated kinase 3 reveals new structural features and insights into its auto-phosphorylation (2018), J. Mol. Biol., 430, 1521-1530 .
    View publication on PubMed

Crystallization (Commentary)

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

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

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

Organism UniProt Comment Textmining
Homo sapiens O43781
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein residue S350 is a phosphorylation site Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + PRAS40 i.e. proline rich Akt substrate 40 Homo sapiens ADP + phosphorylated PRAS40
-
?

Synonyms

Synonyms Comment Organism
dual specificity tyrosine-phosphorylation-regulated kinase 3
-
Homo sapiens
DYRK3
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Homo sapiens

Temperature Stability [°C]

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