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Research at the interface between chemistry and the -omic sciences and systems biology.
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Paper
Mol. BioSyst., 2008, 4, 542 - 550, DOI: 10.1039/b720014e
Design, synthesis and characterization of
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4-anilinoquinazoline kinase inhibitorsB. Gayani K. Perera and Dustin J. Maly
Immobilized kinase inhibitors have emerged as powerful reagents for the determination of kinase inhibitor selectivity and for the enrichment of protein targets from cellular lysates. Here, we report the design and synthesis of a set of
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4-anilinoquinazoline kinase inhibitors. We demonstrate that the attachment of a flexible tether that contains a bio-orthogonal azide functionality does not adversely affect the potency or selectivity of these inhibitors. Furthermore, we demonstrate the utility of these inhibitors through the generation of an affinity matrix for the enrichment of interacting proteins from cellular lysates.
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