Quinone Replacements for Small Molecule Insulin Mimics
نویسندگان
چکیده
منابع مشابه
A Novel Small Molecule 1,2,3,4,6-penta-O-galloyl-α-D-glucopyranose Mimics the Antiplatelet Actions of Insulin
BACKGROUND We have shown that 1,2,3,4,6-penta-O-galloyl-α-D-glucopyranose (α-PGG), an orally effective hypoglycemic small molecule, binds to insulin receptors and activates insulin-mediated glucose transport. Insulin has been shown to bind to its receptors on platelets and inhibit platelet activation. In this study we tested our hypothesis that if insulin possesses anti-platelet properties then...
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Prostate cancer is the second common leading cause of cancer deaths in men worldwide. Medical castration is the standard-care treatment for metastatic prostate cancer patients. Aggressive prostate cancers have a progressive and morbid disease process with a median survival of 9–30 months (Nabhan et al., 2011; Liu and Zhang, 2013). Androgendeprivation therapy (ADT) puts prostate cancer in remiss...
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In type 2 diabetes, impaired insulin signaling leads to hyperglycemia and other metabolic abnormalities. To study a new class of antidiabetic agents, we compared two small, nonpeptide molecules that activate insulin receptor (IR) beta-subunit tyrosine kinase activity: Merck L7, a direct IR agonist, and Telik's TLK16998, an IR sensitizer. In rat hepatoma cells (HTCs) that overexpress the IR (HTC...
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Oral hypoglycemic agents have great potential for the treatment of both type 1 and type 2 diabetes. Here we report the identification of novel, small-molecule, insulin mimetics that activate the insulin receptor (IR) in vivo and in vitro, stimulate the Akt and extracellular signal-regulated kinase pathways downstream of the IR, and mimic the ability of insulin to stimulate glucose uptake, glyco...
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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 like...
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ژورنال
عنوان ژورنال: ChemBioChem
سال: 2008
ISSN: 1439-4227,1439-7633
DOI: 10.1002/cbic.200700597