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Targeting B-cell receptor signaling kinases in chronic lymphocytic leukemia: the promise of entospletinib.


ABSTRACT: The B-cell receptor signaling pathway has emerged as an important therapeutic target in chronic lymphocytic leukemia and other B-cell malignancies. Novel agents have been developed targeting the signaling enzymes spleen tyrosine kinase (SYK), Bruton's tyrosine kinase, and phosphoinositide 3-kinase delta. This review discusses the rationale for targeting these enzymes, as well as the preclinical and clinical evidence supporting their role as therapeutic targets, with a particular focus on SYK inhibition with entospletinib.

SUBMITTER: Sharman J 

PROVIDER: S-EPMC4872176 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature

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Targeting B-cell receptor signaling kinases in chronic lymphocytic leukemia: the promise of entospletinib.

Sharman Jeff J   Di Paolo Julie J  

Therapeutic advances in hematology 20160317 3


The B-cell receptor signaling pathway has emerged as an important therapeutic target in chronic lymphocytic leukemia and other B-cell malignancies. Novel agents have been developed targeting the signaling enzymes spleen tyrosine kinase (SYK), Bruton's tyrosine kinase, and phosphoinositide 3-kinase delta. This review discusses the rationale for targeting these enzymes, as well as the preclinical and clinical evidence supporting their role as therapeutic targets, with a particular focus on SYK inh  ...[more]

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