Aptamers are synthetic RNA or DNA oligonucleotide ligands with a huge potential for therapeutic applications. A vast number of disease-related targets have been used to identify antagonistic, agonistic, and inhibitory aptamers. Armed with a deeper understanding of aptamer structure, target interactions, and pharmacokinetics, Creative Biolabs strongly believes that we are competent to catch up to the preclinical market to offer diverse therapeutic aptamer candidates to promote your drug research project.
Aptamers are a class of potential therapeutic agents due to their synthetic nucleic acid-based nature, their selective and high affinity interaction with target antigens. Therapeutic aptamers are either selected in vitro by using purified proteins, whole cells, tissue or directly in vivo using suitable model systems. Depending on the desired function, the systematic evolution of ligands by exponential enrichment (SELEX) conditions can be adjusted accordingly. For therapeutic applications, aptamers are normally in competition with antibodies and small molecules. As Table 1 shown, aptamers targeting different antigens have been developed with obvious therapeutic applications.
Table 1. Aptamers to partial targets of therapeutic interest. (Keefe, 2010)
| Target | Therapeutic applications | Target | Therapeutic applications |
| α-thrombin | Prevent thrombosis | FGF2 | Prevent angiogenesis |
| HIV-1 Rev | Inhibit viral replication | IgE | Prevent allergies |
| VEGF | Prevent neovascularization | Tenascin C | Prevent tumour development |
| PDGF | Prevent tumor development | αvβ3 integrin | Prevent tumour development |
| l-Selectin | Modulate inflammation | PSMA | Treat progressive malignant prostate disease |
| Interferon-γ | Modulate inflammation and immune response | U1A | Modulate gene regulation |
| Neutrophil elastase | Modulate inflammation | GNRH1 | Prevent tumour development |
| P-selectin | Inhibit viral adhesion | E2F transcription factor | Prevent tumour development |
| Acetylcholine receptor | Control neurotransmission | Neurotensin 1 | Prevent viral infection |
Having worked on adapters for many years with rich experience and sound strategies, Creative Biolabs makes full use of advantages to overcome current challenges such as short half-life in vivo, immunogenicity, and entrapment in cellular organelles. Similar to monoclonal antibodies (mAbs), aptamers can theoretically be used therapeutically in any disease for which extracellular blockade of protein-protein interactions is required. At Creative Biolabs, aptamers can be addressed to intracellular targets, membrane components, or circulating molecules. They can also be used as drug-delivery agents to cells of interest.
On the other hand, wild-type aptamers are too susceptible to nuclease-mediated degradation to be useful for most therapeutic applications. Therefore, chemical modification is necessary to obtain a promising candidate.
Figure.1 Chemical modification of aptamers. (Han, 2020)
Aptamers constitute a new class of oligonucleotides that have gained therapeutic importance. At Creative Biolabs, aptamers could be truncated to reduce synthesis costs, modified at the sugars and capped at their termini to increase nuclease resistance, and conjugated to polyethylene glycol or another entity to reduce renal filtration rates. If you are interested in our therapeutic aptamer agent development to support your research projects, please feel free to contact us.
References
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