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.