Small-molecule inhibitors of spleen tyrosine kinase as therapeutic agents for immune disorders: will promise meet expectations?

作者: Matthew C Lucas , Seng-Lai Tan

DOI: 10.4155/FMC.14.126

关键词: ReceptorPharmacologyMedicineIbrutinibFc receptorImmune systemBruton's tyrosine kinaseTofacitinibProtein kinase ASyk

摘要: Following on the heels of US FDA approval tofacitinib (Xeljanz, Pfizer, USA), an inhibitor JAK family members, and ibrutinib (Imbruvica, Janssen, Belgium), BTK, for treatment rheumatoid arthritis chronic lymphocytic leukemia, respectively, there is now renewed interest in biopharmaceutical industry development orally active small-molecule agents targeting key protein kinases implicated immune regulation. One such ‘immunokinase’ target SYK, a non-receptor tyrosine kinase critical transducing intracellular signaling cascades various recognition receptors, as B-cell receptor Fc receptor. Here, we review discuss progress challenges inhibitors SYK their potential new class disease-modifying immunosuppressive certain inflammatory autoimmune disorders.

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