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

作者：Kamaruddin Mohd Aizuddin; Ung Phuc; Hossain Mohammed Iqbal; Jarasrassamee Boonyarin; O'Malley William; Thompson Philip; Scanlon Denis; Cheng Heung Chin; Graham Bim^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(1): 329-331.

DOI：10.1016/j.bmcl.2010.11.005

• Fluorescence assays
• Click chemistry
• Tyrosine kinases
• Peptides

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.

• 出版日期2011-1