Macromolecular Interactions: Aptamers

AbstractShort nucleic acids can fold into unique three‐dimensional configurations, known as aptamers, to elicit binding of a specific target. The structure of an aptamer, such as stem‐loops, g‐quadruplexes and pseudoknots, directs its ability to recognise and discriminate specific targets. There are significant advantages to aptamers over antibodies, including ease and cost of production as well as lack of immunogenicity. Traditionally, aptamers have been generated by systematic evolution of ligands by exponential enrichment. Aptamers have been developed against a range of targets including proteins, small molecules, intracellular targets, cell‐surface receptors and whole cells, and have thus far resulted in one Food and Drug Administration‐approved therapeutic. Although technical challenges as well as a restrictive intellectual property landscape have hindered the progress of aptamers for direct therapeutic use, they have gained applications as conjugate vehicles for targeted delivery of other therapeutic molecules, in molecular imaging, and as biosensors in increasingly sophisticated detection and monitoring devices.Key Concepts:Nucleic acid aptamers specifically bind a target molecule, including proteins and small molecules, serving as the functional equivalent of chemical antibodies.Aptamers can adopt a multitude of unique three‐dimensional configurations that are required for specific binding of targets.Aptamers are superior to antibodies with regard to ease of production and lack of immunogenicity.Aptamers are traditionally discovered using systematic evolution of ligands by exponential enrichment.Aptamers have been used for a variety of applications including direct therapeutics, vehicles for targeted delivery of compounds, biosensors, diagnostic imaging and nanomachinery.