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Literature summary extracted from

  • Goeckler, N.; Jofre, G.; Papadopoulos, C.; Soppa, U.; Tejedor, F.J.; Becker, W.
    Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation (2009), FEBS J., 276, 6324-6337.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.12.1 expressed in Escherichia coli BL21(DE3) cells Homo sapiens
2.7.12.1 the catalytic domain of DYRK1A is expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.12.1 harmine potent and specific inhibitor of DYRK1A both in vitro and in cultured cells, harmine inhibits DYRK1A substrate phosphorylation more potently than it inhibits tyrosine autophosphorylation; potent and specific inhibitor of DYRK1A, inhibits DYRK1A substrate phosphorylation more potently than it inhibits tyrosine autophosphorylation Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.12.1 ATP + SF3B1 protein-L-Thr434 Homo sapiens
-
 ADP + [SF3B1 protein]-L-Thr434 phosphate
-
 ?
2.7.12.1 ATP + splicing factor 3B1 Homo sapiens splicing factor 3B1 is poshorylated at Thr434 ADP + phosphorylated splicing factor 3B1
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.12.1 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.12.1 glutathione-Sepharose column chromatography Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.12.1 HEK-293 cell
-
 Homo sapiens
-
2.7.12.1 HeLa cell
-
 Homo sapiens
-
2.7.12.1 hippocampus
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.12.1 ATP + SF3B1 protein-L-Thr434
-
 Homo sapiens ADP + [SF3B1 protein]-L-Thr434 phosphate
-
 ?
2.7.12.1 ATP + splicing factor 3B1 splicing factor 3B1 is poshorylated at Thr434 Homo sapiens ADP + phosphorylated splicing factor 3B1
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.12.1 dual-specificity protein kinase
-
 Homo sapiens
2.7.12.1 DYRK1A
-
 Homo sapiens
2.7.12.1 DYRK1A isoform Homo sapiens
2.7.12.1 DYRK1B isoform Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.12.1 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.12.1 0.000033
-
 in 25 mM HEPES, pH 7.0, 5 mM MgCl2, 0.5 mmM dithiothreitol, at 30°C Homo sapiens harmine
2.7.12.1 0.000033
-
 isoform DYRK1A Homo sapiens harmine
2.7.12.1 0.000166
-
 isoform DYRK1B Homo sapiens harmine