The Btk inhibitor LFM-A13 is a potent inhibitor of Jak2 kinase activity
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Abstract
LFMA13, or α-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, was shown to inhibit Brutons tyrosine kinase (Btk). Here we show that LFM-A13 efficiently inhibits erythropoietin (Epo)-induced phosphorylation of the erythropoietin receptor, Janus kinase 2 (Jak2) and downstream signalling molecules. However, the tyrosine kinase activity of immunoprecipitated or in vitro translated Btk and Jak2 was equally inhibited by LFM-A13 in in vitro kinase assays. Finally, Epo-induced signal transduction was also inhibited in cells lacking Btk. Taken together, we conclude that LFM-A13 is a potent inhibitor of Jak2 and cannot be used as a specific tyrosine kinase inhibitor to study the role of Btk in Jak2-dependent cytokine signalling.
Copyright © 2004 by Walter de Gruyter GmbH & Co. KG
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Artikel in diesem Heft
- Publishers Note
- Role of reporter gene imaging in molecular and cellular biology
- Comprehensive search for cysteine cathepsins in the human genome
- Structure of the Q237W mutant of HhaI DNA methyltransferase: an insight into protein-protein interactions
- Identification of arginine residues important for the activity of Escherichia coli signal peptidase I
- Characterization of pancreatic ERj3p, ahomolog of yeast DnaJ-like protein Scj1p
- Carbohydrate moieties can induce mediator release: a detailed characterization of two major timothy grass pollen allergens
- The Btk inhibitor LFM-A13 is a potent inhibitor of Jak2 kinase activity
- Activation of NF-κB/Rel transcription factors in human primary peripheral blood mononuclear cells by interleukin 7
- Cystatin SA, a cysteine proteinase inhibitor, induces interferon-γ expression in CD4-positive T cells
- Inhibition of human pancreatic proteinases by human plasma α2-antiplasmin and antithrombin
- New protease inhibitors from buckwheat seeds: properties, partial amino acid sequences and possible biological role
- Synthesis and antiplasmodial activity of a cysteine protease-inhibiting biotinylated aziridine-2,3-dicarboxylate
- Cathepsins K, L, B, X and W are differentially expressed in normal and chronically inflamed gastric mucosa
