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Small-molecule inducers of insulin expression in pancreatic alpha-cells.
|Publication Type||Journal Article|
|Authors||Fomina-Yadlin, D., Kubicek S., Walpita D., Dancik V., Hecksher-Sørensen J., Bittker JA, Sharifnia T., Shamji A., Clemons PA, Wagner BK, and Schreiber SL|
|Abstract||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.|
|Year of Publication||2010|
|Journal||Proceedings of the National Academy of Sciences of the United States of America|
|Date Published (YYYY/MM/DD)||2010/08/24|