title: 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.
authors.affiliation: Willamette Valley Cancer Institute and Research Center, US Oncology Research, 3377 Riverbend Drive, Suite 500, Springfield, OR 97477, USA.
authors.forename: Jeff
authors.initials: J
authors.lastname: Sharman
authors.affiliation: Department of Biology, Gilead Sciences, Inc., Foster City, CA, USA.
authors.forename: Julie
authors.initials: J
authors.lastname: Di Paolo
keywords: B-cell receptor signaling inhibitors; chronic lymphocytic leukemia; entospletinib; idelalisib; lymphoid malignancies; phosphoinositide 3-kinase delta; spleen tyrosine kinase inhibitors