Over the last three decades, aptamers have been extensively studied for their myriads of applications in clinical research. Aptamers are target-specific ligand molecules which bind selectively to their cognate targets with better affinity than the protein antibodies used in immunotherapeutic approaches for cancer treatment. These short single-stranded stretches of oligonucleotides possess a stable three-dimensional structure which imparts high thermal stability, increased binding affinity and specificity, ease of biochemical synthesis with minimum batch variance, negligible toxicity and immunogenicity and in some cases the ability to penetrate the blood-brain barrier as well. Consequently, they have been comprehensively studied for diverse diagnostic and therapeutic applications, especially in oncology. The use of aptamers for cancer diagnosis and their applications in biomarker discovery are discussed elaborately in the present review. Aptamers can be used in a plethora of ways to target the neoplastic cells directly or indirectly and eventually inhibiting their proliferation. This review focuses on the strategies in which aptamers can be generated in a target-specific manner for cancer therapy, their advantages over the immunotherapeutic methods and their effects on various aspects of cancer therapy. Information pertaining to the aptamers that are currently under clinical trials or have already qualified them is also included in the review.
Keywords: aptamers; aptasensors; biomarkers; cancer; diagnosis; treatment.
© 2025 Wiley‐VHCA AG, Zurich, Switzerland.