Scientific Publications

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

Publication TypeJournal Article
AuthorsFomina-Yadlin, D., Kubicek S., Walpita D., Dancik V., Hecksher-Sørensen J., Bittker JA, Sharifnia T., Shamji A., Clemons PA, Wagner BK, and Schreiber SL
AbstractHigh-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 Publication2010
JournalProceedings of the National Academy of Sciences of the United States of America
Volume107
Issue34
Pages15099-104
Date Published (YYYY/MM/DD)2010/08/24
ISSN Number0027-8424
DOI10.1073/pnas.1010018107
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/20696901?dopt=Abstract