Aptamers as targeted therapeutics: current potential and challenges

By Jiehua Zhou, John J. Rossi. Nature reviews. Drug discovery, 2016

1,793 citations recorded by the source corpus.

Nucleic acid aptamers, often termed 'chemical antibodies', are functionally comparable to traditional antibodies, but offer several advantages, including their relatively small physical size, flexible structure, quick chemical production, versatile chemical modification, high stability and lack of immunogenicity. In addition, many aptamers are internalized upon binding to cellular receptors, making them useful targeted delivery agents for small interfering RNAs (siRNAs), microRNAs and conventional drugs. However, several crucial factors have delayed the clinical translation of therapeutic aptamers, such as their inherent physicochemical characteristics and lack of safety data. This Review discusses these challenges, highlighting recent clinical developments and technological advances that have revived the impetus for this promising class of therapeutics.

Subfields: Biomedical Engineering, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/9b00b3fb24ceded15970f8642b522ab5de1df5a9

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Biomedical Engineering

1. Bo-Shiun Lai
2. Yang Zhang
3. Mario Juhas

In Molecular Biology

1. Bo-Shiun Lai
2. M. Manoharan
3. Martin Egli
4. Yuzong Chen
5. Yang Zhang
6. Mario Juhas

Citations in the corpus

• Nanomedicine in cancer therapy (2023, methodology): “211,212 Although conventional SELEX has proved to be a powerful tool for aptamer selection since its invention in 1990, several important advances, which include the introduction of negative-SELEX and counter-SELEX, the incorporation of magnetic beads, capillary electrophoresis (CE), fl ow…”
• Chemistry, structure and function of approved oligonucleotide therapeutics (2023, background): “About a dozen aptamer therapeutic candidates are currently being evaluated in clinical trials (379,405).”
• Undulating changes in human plasma proteome profiles across the lifespan (2019, neutral): “Currently, one of the most advanced tools for the measurement of plasma proteins is the single ‐ stranded oligonucleotide known as aptamer 17,18 , which binds its target with high affinity and specificity.”
• Aptamers in the Therapeutics and Diagnostics Pipelines (2018, background): “In recent years, several attempts have been made to summarize the existing information about therapeutic aptamers [17-19].”
• Therapeutic target database 2020: enriched resource for facilitating research and early development of targeted therapeutics (2019, background): “The expanded knowledge has facilitated the successful development of new therapies (68), and it will further facilitate the discoveries of such therapeutic approaches as polypharmacology (80) and RNA therapeutics (81).”
• Three decades of nucleic acid aptamer technologies: Lessons learned, progress and opportunities on aptamer development. (2019, background): “The serum half-life of which could be as short as several seconds (Zhou and Rossi, 2016).”
• Recent Advances in Aptamer Discovery and Applications (2019, methodology): “Aptamers have been used successfully for the delivery of a variety of therapeutic reagents into the target cells and tissues [9].”