A facile, click chemistry-based approach to assembling fluorescent chemosensors for protein tyrosine kinases
Date
2011
Authors
Kamaruddin, M.
Ung, O.
Hossain, M.
Jarasrassamee, B.
O'Malley, M.
Thompson, P.
Scanlon, D.
Cheng, H.
Graham, B.
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Journal article
Citation
Bioorganic and Medicinal Chemistry Letters, 2011; 21(1):329-331
Statement of Responsibility
Mohd Aizuddin Kamaruddin, Phuc Ung, Mohammed Iqbal Hossain, Boonyarin Jarasrassamee, William O'Malley, Philip Thompson, Denis Scanlon, Heung-Chin Cheng, Bim Graham
Conference Name
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.
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Crown Copyright © 2010 Published by Elsevier Ltd. All rights reserved.