Microarray-Assisted High-Throughput Identification of a Cell-Permeable Small-Molecule Binder of 14-3-3 Proteins


  • Funding was provided by the Agency for Science, Technology and Research (R-143-000-391-305) and the Ministry of Education (R-143-000-394-112).


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The way to a 14-3-3 binder: A fragment-based combinatorial small-molecule microarray generates affinity-based fingerprints of the 14-3-3σ protein. One small molecule (see picture; in red box) that disrupts the 14-3-3/protein interaction (green/blue) has been identified. The compound is cell-permeable and possesses both in vitro and in-cell activities.