Literature DB >> 20696901

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

Dina Fomina-Yadlin1, Stefan Kubicek, Deepika Walpita, Vlado Dancik, Jacob Hecksher-Sørensen, Joshua A Bittker, Tanaz Sharifnia, Alykhan Shamji, Paul A Clemons, Bridget K Wagner, Stuart L Schreiber.   

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.

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Year:  2010        PMID： 20696901      PMCID： PMC2930573          DOI： 10.1073/pnas.1010018107

Source DB:  PubMed          Journal:  Proc Natl Acad Sci U S A        ISSN： 0027-8424            Impact factor:   11.205


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