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Fluorescent Visualization of Src Using Dasatinib-BODIPY #MMPMID24828915
Vetter ML; Zhang Z; Liu S; Wang J; Cho H; Zhang J; Zhang W; Gray NS; Yang PL
Chembiochem 2014[Jun]; 15 (9): 1317-24 PMID24828915show ga
Many biological experiments are not compatible with the use of immunofluorescence or genetically-encoded fluorescent tags or FRET-based reporters. Conjugation of existing kinase inhibitors to cell-permeable fluorophores can provide a generalized approach to develop fluorescent probes of intracellular kinases. Here, we report the development of a small molecule probe of Src through conjugation of BODIPY to two well-established, dual Src-Abl kinase inhibitors, dasatinib and saracatinib. We show that this approach is not successful for saracatinib, but that largely dasatinib-BODIPY retains the biological activity of its parent compound and can be used to monitor the presence of Src kinase in individual cells by flow cytometry and to track the localization of Src by fixed and live-cell fluorescence microscopy. This strategy may enable generation of additional kinase-specific probes useful in systems not amenable to genetic manipulation or used together with fluorescent proteins to enable a multiplexed assay read-out.