论文部分内容阅读
尽管许多基因组靶标的功能及它们与疾病的关系仍然不清楚 ,但基因组信息的获得仍极大地丰富了潜在药物靶标的数量。在化学基因组学研究中 ,基因组靶标超高通量筛选发生在药物开发的初期 ,在确定靶标之前进行。靶标选择性调控剂可提供药物先导结构和药理学研究工具以鉴定靶标功能 ,化学基因组策略的有效实施离不开能对大量基因组靶标进行超高通量筛选的分析检测技术的运用。基于细胞功能的分析实验可以实现化学基因组学研究中超高通量筛选的目的 ,并且因其功能特性使其在鉴定靶标选择性调控剂时明显优于配体结合试验
Although the function of many genomic targets and their relationship to disease remains unclear, the availability of genomic information has greatly enriched the number of potential drug targets. In chemical genomics studies, genomic target ultra-high throughput screening occurs early in drug development and before targeting. Targeted selective modulators provide drug lead structures and pharmacological research tools to identify target functions. The effective implementation of chemical genomic strategies can not be separated from the use of analytical assays that enable ultra-high throughput screening of a large number of genomic targets. Cell-based assays enable ultra-high-throughput screening in chemical genomics and their functional properties make them significantly superior to ligand binding assays in identifying target selective modulators