Abstract

The invention of the in vitro selection technique, or SELEX (Systematic Evolution of Ligands by EXponential enrichment), in the early 1990s, identified single-stranded (ss) nucleic acid molecules with catalytic or binding properties from random-sequence nucleic acid libraries.1–3 This technique has given rise to intensive examinations of synthetic functional nucleic acids (aptamers and nucleic acid enzymes) for wide-ranging applications including biosensors, diagnostics and therapeutics.4–9After nearly three decades of research by many groups around the world, many functional nucleic acids have been isolated and characterized. A few well-known examples are provided in Figure 1, including two RNA-cleaving DNAzymes (8-17 and 10-23),10 a peroxidase-mimicking DNAzyme (PS2.M),11 two DNA aptamers that bind human α-thrombin (TBA15 and TBA29),12,13 a DNA aptamer that binds ATP,14 and a modified nucleic acid aptamer that binds human VEGF-165 (Pegaptanib).15 Thousands of papers have been published describing the us...

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