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

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.

DOI: 10.1073/pnas.1010018107

3 Figures and Tables

05010020102011201220132014201520162017
Citations per Year

312 Citations

Semantic Scholar estimates that this publication has 312 citations based on the available data.

See our FAQ for additional information.

Cite this paper

@article{FominaYadlin2010SmallmoleculeIO, title={Small-molecule inducers of insulin expression in pancreatic alpha-cells.}, author={Dina Fomina-Yadlin and Stefan Kubicek and Deepika Walpita and Vlado Danc{\'i}k and Jacob Hecksher-S\orensen and Joshua A. Bittker and Tanaz Sharifnia and Alykhan F. Shamji and Paul A. Clemons and Bridget K Wagner and Stuart L. Schreiber}, journal={Proceedings of the National Academy of Sciences of the United States of America}, year={2010}, volume={107 34}, pages={15099-104} }