Blank Michael, Blind Michael
NascaCell IP GmbH, München, Germany.
Curr Opin Chem Biol. 2005 Aug;9(4):336-42. doi: 10.1016/j.cbpa.2005.06.011.
Synthetic nucleic acid ligands, called aptamers, bind to protein targets with high specificity and affinity. They are very potent inhibitors of protein function and their application can greatly enhance the process of target validation and drug development. An important benefit of this technology is the recent development of rapidly identifying these sophisticated ligands for almost any target molecule in multi-parallel, automated workstations. The aptamer technology is thus well-suited to addressing the growing demand for high-throughput analysis and functional validation of potential drug targets. Numerous examples have shown the potency of aptamers in inhibiting the function of proteins in cell culture and in vivo models. The technology is complementary to genetic knockout or siRNA approaches as it provides highly valuable information at the proteomic level. In addition, the aptamer technology has recently been extended to developing aptamer drugs and identifying functionally equivalent small molecule leads.
合成核酸配体，即适体，能以高特异性和亲和力与蛋白质靶点结合。它们是蛋白质功能的强效抑制剂，其应用能够极大地促进靶点验证和药物研发进程。这项技术的一个重要优势是近期在多平行自动化工作站中快速识别几乎任何靶分子的这些精密配体方面取得的进展。因此，适体技术非常适合满足对潜在药物靶点进行高通量分析和功能验证日益增长的需求。大量实例表明适体在细胞培养和体内模型中抑制蛋白质功能的效力。该技术与基因敲除或RNA干扰方法互补，因为它在蛋白质组水平提供了极具价值的信息。此外，适体技术最近已扩展到开发适体药物和识别功能等效的小分子先导物。
