Literature summary for 2.7.10.2 extracted from

Hantschel, O.; Rix, U.; Schmidt, U.; Buerckstuemmer, T.; Kneidinger, M.; Schuetze, G.; Colinge, J.; Bennett, K.L.; Ellmeier, W.; Valent, P.; Superti-Furga, G.
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib (2007), Proc. Natl. Acad. Sci. USA, 104, 13283-13288.

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Inhibitors

Inhibitors	Comment	Organism	Structure
dasatinib	i.e. BMS-354825, a Bcr-Abl inhibitor, used for the treatment of imatinib-resistant chronic myelogenous leukemia, inhibits Abl and Src kinases, and the Tec kinases Btk at Th474 and Tec at Thr442, but not Itk, the mutant BtkT474I ans TecT442I are resistant to dasatinib, while mutantion of the insensitive wild-type Itk to ItkF435T renders the enzyme sensitive to dasatinib, overview, autophosphorylation of Btk at Tyr223 is inhibited only by dasatinib but not by imatinib or nilotinib	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
phosphoprotein	Btk performs autophosphorylation on Tyr223, which is inhibited only by dasatinib but not by imatinib or nilotinib	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
JURKAT cell	-	Homo sapiens	-
K-562 cell	-	Homo sapiens	-
NAMALWA cell	-	Homo sapiens	-
U-937 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + biotin-GGEAIYAAPFKK-amide	a peptide with the preferred c-Abl substrate sequence carrying an Nterminal biotin	Homo sapiens	ADP + phosphorylated biotin-GGEAIYAAPFKK-amide	-	?
additional information	Btk performs autophosphorylation on Tyr223	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
Abl kinase	-	Homo sapiens
Btk	-	Homo sapiens
Btk tyrosine kinase	-	Homo sapiens
Src kinase	-	Homo sapiens
Tec	-	Homo sapiens
Tec kinase	-	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.5	-	assay at	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000005	-	inhibition of Btk kinase, pH 7.5	Homo sapiens	dasatinib
0.000014	-	inhibition of Abl kinase, pH 7.5	Homo sapiens	dasatinib
0.000228	-	inhibition of Itk F435T kinase mutant, pH 7.5	Homo sapiens	dasatinib
0.000297	-	inhibition of Tec kinase, pH 7.5	Homo sapiens	dasatinib

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Release 2023.1 (January 2023)