This week’s HOT paper comes from Priscilla Yang and colleagues at Harvard and the University of Massachusetts Boston, who have developed small molecule tools for imaging kinases by fluorescence microscopy.
In their communication, the team synthesised fluorophore-conjugated derivatives of the PLK inhibitor BI2536 and the Mps1 inhibitor Mps1-IN-1. Although the conjugation of BI2536 with BODIPY resulted in a compound that displayed similar biochemical and cellular properties as the original inhibitor, the conjugation of Mps1-IN-1 with BODIPY disrupted the interaction of the inhibitor with its target – therefore, only the BI-BODIPY compound was used for imaging. The team were able to show BI-BODIPY as a cell permeable probe, using fluorescence microscopy to image the localisation of PLK in cells.
The authors state that the study shows proof of concept ‘to convert other small molecule kinase inhibitors to probes that can analogously be used to monitor localisation of their respective kinases’.
Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy
Zijuan Zhang, Nicholas Kwiatkowski, Hong Zeng, Sang Min Lim, Nathanael S. Gray, Wei Zhang and Priscilla L. Yang
DOI: 10.1039/C2MB25099C
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