Development of a simple screening system for the discovery of a new drug for diabetes

有500多万糖尿病患者，必须开发一种新的口服药物。然而，目前还没有一种简单、定量的方法来寻找口服糖尿病药物。整个动物都在寻找新的药物来估计降糖作用，但这种方法并不能大量筛选化合物。4型葡萄糖转运体(GLUT4)从细胞内池转移到细胞表面是胰岛素刺激胰岛素靶细胞摄取葡萄糖的主要机制。我们利用c-myc表位标记的GLUT4(GLUT4myc)，建立了一种高灵敏度、定量检测完整细胞表面GLUT4的方法。我们建立了在CHO、L6成肌细胞和3T3L1脂肪细胞中表达GLUT4myc的稳定克隆。我们开发了一种简单而新的方法来筛选触发GLUT4myc易位的化合物，该方法在96个井中使用。这种方法对于开发治疗糖尿病的新药的首次筛选是有用的。

There are more than 5 million patients of diabetes and a new oral drug must be developed. However, there is not a simple and quantitative method to find the oral diabetic drug. Whole animal was used to find the new drug to estimate the decrease of blood glucose level, but this method is not adeguate toscreen a large number of compound. Translocation of the type 4 glucose transporter (GLUT4) to the cell surface from an intracellular pool is the major mechanism of insulin-stimulated glucose uptake in insulin-target cells. We developed a highly sensitive and quantitative method of detect GLUT4 immunologically on the surface of intact cells, using c-myc epitope-tagged GLUT4 (GLUT4myc). We established stable clones to express GLUT4myc in CHO,L6 myoblasts and 3T3L1 adipocytes. We have developed a simple and new method to screen the compounds for triggering the GLUT4myc translocation in 96 wells using luminessence method. This method is useful for the first screening for developing a new oral drug for diabetes.