☆ 4.4 Article

Flow Cytometric Determination of Src Phosphorylation in Pediatric Patients Treated With Dasatinib

PEDIATRIC BLOOD & CANCER (2009)

Journal

PEDIATRIC BLOOD & CANCER

Volume 53, Issue 6, Pages 1132-1135

Publisher

WILEY

DOI: 10.1002/pbc.22083

Keywords

clasatinib; phase I; Src kinases; tyrosine kinase inhibitor

Categories

Oncology Hematology Pediatrics

Funding

NIH Leukemia SPORE P50 [CA 100632]

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Abstract

Tyrosine kinase inhibitors, such as imatinib, have dramatically improved the outcomes for patients with selected cancers. For imatinib, western blotting of phospho-CrkL was an insensitive, indirect, and descriptive method to determine drug efficacy. Greater use of targeted therapies should involve more quantitative evaluation of the target's dose-inhibition. The Src/Abl kinase inhibitor dasatinib has recently been approved for use in Ph+ leukemias after failure with imatinib. Src family kinases (SFK) also play a critical role in nonhematologic cancers. We have developed a flow cytometric assay to measure SFK autophosphorylation levels in blood mononuclear cells and observed a direct correlation between its inhibition and patient dosage. This method provides a sensitive, quick, and quantitative tool to assess drug efficacy. Pediatr Blood Cancer 2009;53:1132-1135. (C) 2009 Wiley-Liss, Inc.

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