A facile, click chemistry-based approach to assembling fluorescent chemosensors for protein tyrosine kinases.

Abstract	A group of fluorophore-labeled peptide substrates of Src kinases have been synthesized with the aid of click chemistry. Some of the generated peptides exhibit an increase in fluorescence upon phosphorylation and are capable of detecting Src kinases with high sensitivity and specificity. Their availability permits real-time activity measurement of aberrantly activated oncogenic Src kinases in the crude lysate of chronic myelogenous leukemia cells. These new chemosensor peptides are highly useful tools that can be used for high-throughput screening to search for small molecule inhibitors of Src kinases as potential therapeutics for cancer treatment.
Authors	Mohd Aizuddin Kamaruddin, Phuc Ung, Mohammed Iqbal Hossain, Boonyarin Jarasrassamee, William O'Malley, Philip Thompson, Denis Scanlon, Heung-Chin Cheng, Bim Graham
Journal	Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 21 Issue 1 Pg. 329-31 (Jan 01 2011) ISSN: 1464-3405 [Electronic] England
PMID	21111620 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Copyright	Crown Copyright © 2010. Published by Elsevier Ltd. All rights reserved.
Chemical References	Fluorescent Dyes Peptides src-Family Kinases
Topics	Amino Acid Sequence Biosensing Techniques Cell Line, Tumor Click Chemistry Enzyme Assays (methods) Fluorescent Dyes (chemistry) High-Throughput Screening Assays Humans Peptides (chemistry) Phosphorylation Substrate Specificity src-Family Kinases (metabolism)

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