Syk Inhibitors in Clinical Development for Hematological Malignancies

Authors

Delong Liu, New York Medical CollegeFollow
Aleksandra Mamorska-Dyga

DOI

10.1186/s13045-017-0512-1

Journal Title

Journal of Hematology & Oncology

First Page

145

Document Type

Article

Publication Date

7-28-2017

Department

Medicine

Keywords

Syk, spleen tyrosine kinase, PTK, protein tyrosine kinase, hematopoietic cells, fostamatinib, R788, entospletinib, GS-9973, cerdulatinib, PRT062070

Disciplines

Amino Acids, Peptides, and Proteins | Biochemistry | Enzymes and Coenzymes | Medicine and Health Sciences

Abstract

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.

Recommended Citation

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

Publisher's Statement

Originally published in Journal of Hematology & Oncology, 10 (1), 145. The original material can be found here.

Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 International License.