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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 |
| Volume | 107 |
| Issue | 34 |
| Pages | 15099-104 |
| Date Published (YYYY/MM/DD) | 2010/08/24 |
| ISSN Number | 0027-8424 |
| DOI | 10.1073/pnas.1010018107 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/20696901?dopt=Abstract |
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