Anti-VEGF DNA-based aptamers in cancer therapeutics and diagnostics

The vascular endothelial growth factor (VEGF) family and its receptors play fundamental roles not only in physiological but also in pathological angiogenesis, characteristic of cancer progression. Aiming at finding putative treatments for several malignancies, various small molecules, antibodies, or protein-based drugs have been evaluated in vitro and in vivo as VEGF inhibitors, providing efficient agents approved for clinical use. Due to the high clinical importance of VEGF, also a great number of anti-VEGF nucleic acid-based aptamers-that is, oligonucleotides able to bind with high affinity and specificity a selected biological target-have been developed as promising agents in anticancer strategies. Notable research efforts have been made in optimization processes of the identified aptamers, searching for increased target affinity and/or bioactivity by exploring structural analogues of the lead compounds. This review is focused on recent studies devoted to the development of DNA-based aptamers designed to target VEGF. Their therapeutic potential as well as their significance in the construction of highly selective biosensors is here discussed.

Automated summary

The VEGF family and its receptors are crucial in pathological angiogenesis and cancer progression, leading to the development of potential treatments for malignant tumors. Various VEGF inhibitors, including small molecules, antibodies, and nucleic acid-based aptamers, have been evaluated for clinical use, showing promising therapeutic potential in anticancer strategies. Efforts to optimize these aptamers by increasing target affinity and exploring structural analogues of lead compounds have been made, highlighting their significance in highly selective biosensor construction and therapeutic applications.