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https://hdl.handle.net/2440/72186
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Type: | Journal article |
Title: | A facile, click chemistry-based approach to assembling fluorescent chemosensors for protein tyrosine kinases |
Author: | Kamaruddin, M. Ung, O. Hossain, M. Jarasrassamee, B. O'Malley, M. Thompson, P. Scanlon, D. Cheng, H. Graham, B. |
Citation: | Bioorganic and Medicinal Chemistry Letters, 2011; 21(1):329-331 |
Publisher: | Pergamon-Elsevier Science Ltd |
Issue Date: | 2011 |
ISSN: | 0960-894X 1464-3405 |
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 |
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. |
Keywords: | Fluorescence assays Click chemistry Tyrosine kinases Peptides |
Rights: | Crown Copyright © 2010 Published by Elsevier Ltd. All rights reserved. |
DOI: | 10.1016/j.bmcl.2010.11.005 |
Grant ID: | NHMRC |
Published version: | http://dx.doi.org/10.1016/j.bmcl.2010.11.005 |
Appears in Collections: | Aurora harvest 5 Chemistry publications |
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