Small-molecule inducers of insulin expression in pancreatic α-cells
D Fomina-Yadlin, S Kubicek… - Proceedings of the …, 2010 - National Acad Sciences
Proceedings of the National Academy of Sciences, 2010•National Acad Sciences
High-content screening for small-molecule inducers of insulin expression identified the
compound BRD7389, which caused α-cells to adopt several morphological and gene
expression features of a β-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 β-cell-like state.
BRD7389 also increases the endocrine cell content and function of donor human pancreatic …
compound BRD7389, which caused α-cells to adopt several morphological and gene
expression features of a β-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 β-cell-like state.
BRD7389 also increases the endocrine cell content and function of donor human pancreatic …
High-content screening for small-molecule inducers of insulin expression identified the compound BRD7389, which caused α-cells to adopt several morphological and gene expression features of a β-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 β-cell-like state. BRD7389 also increases the endocrine cell content and function of donor human pancreatic islets in culture.
National Acad Sciences