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

Mohd Kamaruddin, Phuc Ung, Mohammed Hossain, Boonyarin Jarasrassamee, William O'Malley, Philip Thompson, Denis Scanlon, Heung-Chin Cheng, Bimbil Graham

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11 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)329 - 331
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number1
DOIs
Publication statusPublished - 2011

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