Targeted therapeutics underwent a revolution with the entry of monoclonal antibodies in the medical toolkit. Oligonucleotide aptamers form another family of target agents that have been lagging behind in reaching the clinical arena in spite of their potential clinical translation. Some of the reasons for this might be related to the challenge in identifying aptamers with optimal in vivo specificity, and the nature of their pharmacokinetics. Aptamers usually show exquisite specificity, but they are also molecules that display dynamic structures subject to changing environments. Temperature, ion atmosphere, pH, and other variables are factors that could determine the affinity and specificity of aptamers. Thus, it is important to tune the aptamer selection process to the conditions in which you want your final aptamer to function; ideally, for in vivo applications, aptamers should be selected in an in vivo-like system or, ultimately, in a whole in vivo organism. In this review we recapitulate the implementations in systematic evolution of ligands by exponential enrichment (SELEX) to obtain aptamers with the best in vivo activity.

随着单克隆抗体进入医疗工具箱，靶向治疗药物经历了一场革命。寡核苷酸适体形成了另一类靶标药物，尽管它们具有潜在的临床翻译功能，但它们在到达临床领域时仍然落后。某些原因可能与鉴定具有最佳体内适体的挑战有关特异性及其药代动力学的性质。适体通常显示出极好的特异性，但它们也是在变化的环境中表现出动态结构的分子。温度，离子气氛，pH和其他变量是可以确定适体亲和力和特异性的因素。因此，将适配子的选择过程调整到您希望最终适配子起作用的条件非常重要。理想地，对于体内应用，应当在类体内系统中或最终在整个体内生物体中选择适体。在这篇综述中，我们概述了通过指数富集（SELEX）实现配体系统进化的方法，以获得体内最佳的适体 活动。