Small-molecule inducers of insulin expression in pancreatic alpha-cells.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 20696901.
- Also identified by DOI 10.1073/pnas.1010018107 and PMC identifier 2930573.
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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.
Medical subject headings
- Glucagon-Secreting Cells
- Insulin
- Protein Kinase Inhibitors
- Quinolones