'Turn On/Off' fluorescence probe for the screening of unactivated Bruton's tyrosine kinase.

Authors :: Kawahata W
Asami T
Fujii I
Sawa M
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015; Vol. 25 (10), pp. 2141-5. Date of Electronic Publication: 2015 Mar 30.
Publication Year :: 2015
Abstract: BTK has emerged as a promising target for treating B-cell malignancies and autoimmune diseases, and there has been a growing demand to identify selective BTK inhibitors efficiently. In this Letter, we have designed and synthesized a new fluorescent probe to screen compounds that preferentially bind to an unactivated state of BTK (BTK [U]). The fluorescence of the probe was turned on in the presence of BTK [U], and quenched by the addition of compounds which preferentially bind to BTK [U]. This unique fluorescent probe was successfully applied to the screening of a kinase focused compound library. The results suggest that this new method is a simple and easy-to-perform assay to screen inhibitors of BTK [U].<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)

Subjects :: Agammaglobulinaemia Tyrosine Kinase
Protein Kinase Inhibitors pharmacology
Protein-Tyrosine Kinases antagonists & inhibitors
Fluorescent Dyes chemistry
Protein-Tyrosine Kinases analysis

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