Insulin Receptor
The insulin receptor (IR) is a transmembrane receptor that is activated by insulin, IGF-I, IGF-II and belongs to the large class of tyrosine kinase receptors. Metabolically, the insulin receptor plays a key role in the regulation of glucose homeostasis, a functional process that under degenerate conditions may result in a range of clinical manifestations including diabetes and cancer.Tyrosine kinase receptors, including the insulin receptor, mediate their activity by causing the addition of a phosphate group to particular tyrosines on certain proteins within a cell. The "substrate" proteins that are phosphorylated by the Insulin Receptor include a protein called "IRS-1" for "insulin receptor substrate 1". IRS-1 binding and phosphorylation eventually leads to an increase in the high affinity glucose transporter (Glut4) molecules on the outer membrane of insulin-responsive tissues.
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HFI 142是Insulin-regulated aminopeptidase (IRAP) 抑制剂。
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Demethylasterriquinone B1是选择性 insulin RTK 激动剂。
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BRD 7552是PDX1 transcription factor inducer， increases insulin expression。
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NBI 31772是高亲和性 insulin-like growth factor-I binding protein IGFBP的抑制剂。
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Linsitinib(OSI-906)是口服活性的ATP竞争性IGF-1R和insulin受体双重抑制剂，IC50分别为35 nM和75 nM。
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