Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors like Fc receptors and adhesion receptors. Several oral Syk inhibitors including fostamatinib (R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659 are being assessed in clinical trials. The second generation compound, entospletinib, showed promising results in clinical trials against B-cell malignancies, mainly chronic lymphoid leukemia. Syk inhibitors are being evaluated in combination regimens in multiple malignancies.
Liu, D., & Mamorska-Dyga, A. (2017). Syk Inhibitors in Clinical Development for Hematological Malignancies. Journal of Hematology & Oncology, 10 (1), 145. https://doi.org/10.1186/s13045-017-0512-1
Originally published in Journal of Hematology & Oncology, 10 (1), 145. The original material can be found here.
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