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Pyrrolo[1,2‐a]quinoxalines: Insulin Mimetics that Exhibit Potent and Selective Inhibition against Protein Tyrosine Phosphatase 1B
ChemMedChem ( IF 3.4 ) Pub Date : 2020-09-16 , DOI: 10.1002/cmdc.202000710
Javier García‐Marín 1, 2, 3 , Mercedes Griera 2, 4 , Patricia Sánchez‐Alonso 1 , Bruno Di Geronimo 5 , Francisco Mendicuti 3, 6 , Manuel Rodríguez‐Puyol 2, 4 , Ramón Alajarín 1, 2, 3 , Beatriz Pascual‐Teresa 5 , Juan J. Vaquero 1, 2, 3 , Diego Rodríguez‐Puyol 2, 4
Affiliation  

The Front Cover shows a C2C12 cell with the inhibitor 4‐benzylpyrrolo[1,2‐a]quinoxaline targeting the α3/α6/α7 tunnel in the Protein Tyrosine Phosphatase 1B (PTP1B) represented as a ribbon diagram. The insulin receptor (clear green) and the glucose transporter (clear yellow) shown at the cell membrane are involved in the glucose uptake by the cell. The inhibition of PTP1B by this molecule and their analogues produces an insulin mimetic effect. This is indicated by red arrows for the glucose molecules (in sticks) crossing the cell membrane to the cytosol. Cover design by Javier García‐Marín. More information can be found in the Full Paper by Manuel Rodríguez‐Puyol, Ramón Alajarín, Juan J. Vaquero, Diego Rodríguez‐Puyol et al.
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中文翻译:

吡咯并[1,2-a]喹喔啉:对蛋白质酪氨酸磷酸酶1B具有强效和选择性抑制作用的胰岛素模拟物

封面显示了一个C2C12细胞,其抑制剂4-酪氨酸吡咯并[ 1,2-a ]喹喔啉靶向蛋白酪氨酸磷酸酶1B(PTP1B)中的α3/α6/α7通道,以带状图表示。细胞膜上显示的胰岛素受体(透明的绿色)和葡萄糖转运蛋白(透明的黄色)与细胞摄取葡萄糖有关。该分子及其类似物对PTP1B的抑制作用可产生胰岛素模拟作用。红色箭头表示穿过细胞膜到达细胞质的葡萄糖分子(棒状)。封面设计由哈维尔·加西亚·马林(JavierGarcía-Marín)设计。可以在ManuelRodríguez-Puyol,RamónAlajarín,Juan J.Vaquero,DiegoRodríguez-Puyol等人的论文全文中找到更多信息。
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更新日期:2020-10-05
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