Small-molecule inducers of insulin expression in pancreatic alpha-cells.


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.

DOI: 10.1073/pnas.1010018107

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@article{FominaYadlin2010SmallmoleculeIO, title={Small-molecule inducers of insulin expression in pancreatic alpha-cells.}, author={Dina Fomina-Yadlin and Stefan Kubicek and Deepika Walpita and Vlado Danc{\'i}k and Jacob Hecksher-S\orensen and Joshua A. Bittker and Tanaz Sharifnia and Alykhan F. Shamji and Paul A. Clemons and Bridget K Wagner and Stuart L. Schreiber}, journal={Proceedings of the National Academy of Sciences of the United States of America}, year={2010}, volume={107 34}, pages={15099-104} }