Target Validation Information
TTD ID	T62431
Target Name	Tyrosine-protein kinase SYK (SYK)
Type of Target	Successful
Drug Potency against Target	Fostamatinib	Drug Info	Ki = 30 nM	[3]
	ELLAGIC ACID	Drug Info	IC50 = 4300 nM	[2]
	N-Benzyl-4-(2,5-dihydroxy-benzylamino)-benzamide	Drug Info	IC50 = 18000 nM	[1]
Action against Disease Model	Fostamatinib	Drug Info	R788, the oral solid dosage formulation of R406, is a novel syk kinase inhibitor that blocks the activation of mast cells, B cells and macrophages by blocking IgG signaling. In the first study, R788 was found to be protective from immune thrombocytopenia and hemolytic anemia in a mouse model. This study suggests that R788 may be useful in the treatment of Immune Thrombocytopenic Purpura (ITP) as well as improving autoimmune hemolytic anemia (AIHA). In a second study, R406 inhibited t uMor growth in a dose-dependent manner in a xenograft mouse model with a h uMan acute mylelogenous leukemia (AML) FLT3 cell line, demonstrating that R406 may be a beneficial in FLT3-type AML. AML is characterized by the overproduction of immature white blood cells, which causes deficits of other normal blood cells.
References
REF 1	Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin ... J Med Chem. 2001 Feb 1;44(3):441-52.
REF 2	Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. J Med Chem. 2006 Apr 20;49(8):2363-6.
REF 3	R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

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