Aptamers are single-stranded
oligonucleotides that specifically bind and interact with their corresponding targets, including
proteins and cells, through unique three-dimensional structures. Numerous aptamers have been developed to target
cancer biomarkers with high specificity and affinity, and some are employed as versatile guiding
ligands for
cancer-specific drug delivery and anti-
cancer therapeutics. In this review, we list the aptamers that target
tumor surface
biomarkers and summarize the representative applications of aptamers as agonists and antagonists that activate anti-
cancer and inactivate pro-
cancer biomarkers, respectively. In addition, we describe applications of aptamer-drug or aptamer-
oligonucleotide conjugates that can deliver therapeutic agents, including small interfering RNAs, micro RNAs, short hairpin RNAs, and chemotherapeutic molecules, to
cancer cells. Moreover, we provide examples of aptamer- conjugated nano-vehicles, in which
cancer-targeting
oligonucleotide aptamers are conjugated with nano-vehicles such as
liposomes,
micelles, polymeric nanoparticles, and
quantum dots. Conjugation of aptamers with anti-
cancer drugs and nano-vehicles will facilitate innovative applications of aptamer-based
cancer therapeutics.