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  • 标题:Small-molecule inducers of insulin expression in pancreatic α-cells
  • 本地全文:下载
  • 作者:Dina Fomina-Yadlin ; Stefan Kubicek ; Deepika Walpita
  • 期刊名称:Proceedings of the National Academy of Sciences
  • 印刷版ISSN:0027-8424
  • 电子版ISSN:1091-6490
  • 出版年度:2010
  • 卷号:107
  • 期号:34
  • 页码:15099-15104
  • DOI:10.1073/pnas.1010018107
  • 语种:English
  • 出版社:The National Academy of Sciences of the United States of America
  • 摘要:High-content screening for small-molecule inducers of insulin expression identified the compound BRD7389, which caused -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.
  • 关键词:BRD7389 ; pancreatic islets ; Rsk kinase ; transdifferentiation ; beta cells
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