Target identification of bioactive molecules, which leads to the development of novel classes of drugs with few side effects or the discovery of new druggable proteins, is a vital and still daunting task. To overcome the time-consuming work, we developed a novel affinity labeling method employing a small bifunctional O-nitrobenzoxadiazole (O-NBD) unit having both reactivity and potential fluorescence. O-NBD is usually not fluorescent, but gives the fluorescence in response to existing amino group in protein. This method is not only simple but also powerful for target identification as well as ligand binding-site determination. Moreover, since the target labeling takes place with turn-ON fluorescence, the approach enables a sensitive imaging/detection of target proteins in living cells.
The Exploratory Research for Advanced Technology (ERATO)
"Sodeoka Live Cell Chemistry Project"
Takao Yamaguchi, Miwako Asanuma, Shuichi Nakanishi, Yohei Saito,
Masateru Okazaki, Kosuke Dodo, and Mikiko Sodeoka
"Turn-ON fluorescent affinity labeling using a small bifunctional O-nitorobenzoxadiazole unit"
Chem. Sci., 2014, Advance Article
Mikiko Sodeoka Ph.D.
Director of Synthetic Organic Chemistry, RIKEN
Director of ERATO Live Cell Chemistry Project, JST
Department of Research Project
Japan Science and Technology Agency