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Literature summary for 2.7.12.1 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
Search for more literature for 2.7.12.1

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
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)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

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