在药物研发中对具有生物活性的物质进行快速筛选是先导化合物开发的关键技术之一。蛋白激酶、G蛋白偶联受体和离子通道并称药物设计的三大靶点，蛋白激酶抑制剂作为潜在的抗癌、抗肿瘤治疗药物而成为研究的热点。目前的蛋白激酶活性物质筛选方法如稳定同位素法、酶联免疫法、毛细管电泳法和荧光多肽法等都具有一定的局限性。本论文拟发展一种基于γ-[18O4]-ATP稳定同位素结合MALDI-TOF质谱技术的蛋白激酶抑制剂筛选的新方法,该方法具有上述四种筛选法的所有优点：灵敏度高、分析速度快、经济实惠、适用于大规模的药物筛选。 实验以PKA为模型，Kemptide为底物模拟肽，采用非放射性18O稳定同位素标记ATP的...The high-throughput screening of bioactive compounds is the key technique for the discovery of lead compound in medicinal chemistry. Protein kinases, G protein-couple receptors and Ion channels, are the three targets of drug design. Protein kinase inhibitors become focus of research owe to the potential in anti-cancer and anti-tumor. Recently, the methodologies for screening of protein kinase inhi...学位：理学硕士院系专业：化学化工学院_有机化学学号：2052011115160
