Fluorometric assay of integrin activity with a small-molecular probe that senses the binding site microenvironment.
نویسندگان
چکیده
We have developed a small-molecular probe, consisting of cyclic RGD pentapeptides bearing a nitrobenzoxadiazole fluorophore at the 4'-residue, which detects integrin αVβ3 activity in terms of fluorescence intensity decrease due to quenching of the fluorophore by interaction with tyrosine-122 at the binding site of the protein. This probe appears to be suitable for a practical, high-throughput fluorescence assay to screen small-molecular modulators of integrin activity.
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عنوان ژورنال:
- Chemical communications
دوره 50 100 شماره
صفحات -
تاریخ انتشار 2014