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

doi:10.1016/j.bmcl.2010.11.005

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

Medicinal Chemistry

Research output: Contribution to journal › Article › Research › peer-review

13 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 language	English
Pages (from-to)	329 - 331
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2010.11.005
Publication status	Published - 2011

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SDG 3 Good Health and Well-being

Access to Document

10.1016/j.bmcl.2010.11.005

Cite this

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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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AU - Kamaruddin, Mohd

AU - Ung, Phuc

AU - Hossain, Mohammed

AU - Jarasrassamee, Boonyarin

AU - O'Malley, William

AU - Thompson, Philip

AU - Scanlon, Denis

AU - Cheng, Heung-Chin

AU - Graham, Bimbil

PY - 2011

Y1 - 2011

N2 - 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.

AB - 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.

U2 - 10.1016/j.bmcl.2010.11.005

DO - 10.1016/j.bmcl.2010.11.005

M3 - Article

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VL - 21

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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