|Publication Type||Journal Article|
|Year of Publication||2010|
|Authors||Fomina-Yadlin, D, Kubicek, S, Walpita, D, Dancik, V, Hecksher-Sørensen, J, Bittker, JA, Sharifnia, T, Shamji, A, Clemons, PA, Wagner, BK, Schreiber, SL|
|Journal||Proceedings of the National Academy of Sciences of the United States of America|
High-content screening for small-molecule inducers of insulin expression identified the compound BRD7389, which caused alpha-cells to adopt several morphological and gene expression features of a beta-cell state. Assay-performance profile analysis suggests kinase inhibition as a mechanism of action, and we show that biochemical and cellular inhibition of the RSK kinase family by BRD7389 is likely related to its ability induce a beta-cell-like state. BRD7389 also increases the endocrine cell content and function of donor human pancreatic islets in culture.