Aptamer Optimization Services

Creative Biolabs has long-term devoted to aptamer development, optimization, and application. With years of experience, our scientists have tailored hundreds of particular libraries and numbers of specific aptamer products to boost our global customers’ research and project goals.

Aptamer Overview

Dated back to 1990, aptamers are single-strand DNA- or RNA-based oligonucleotides (or peptides) that can selectively bind to various target molecules in high-affinity and high-specificity manners. Aptamers are relatively small molecules with specific tertiary structures, usually consisting of 40 to 180 nucleotides or 10 to 30 amino acid residues, which are synthesized and screened by Systematic Evolution of Ligands by EXponential enrichment (SELEX) in vitro.

In recent years, aptamers serve as valuable tools for a wide range of diagnostic and therapeutic applications. And aptamers are increasingly being developed as alternatives to the antibody for target recognition since they display unique advantages over antibodies.

Table.1 Advantage of aptamers compared with the antibody.

Aptamer Antibody
Size Small (~10-50 kDa) Large (>150 kDa)
Stability Thermal stability and chemical stability Sensitive to temperature and easy denaturation
Affinity High High
Immunogenicity None/Low High
Targets Widely covers proteins, small molecules, cells, ions, toxins, etc. Immunogenic proteins, peptides, and polysaccharides
Tissue penetration Efficient at penetrating tissues and cells Low penetration and internalization efficiency
Modifications Easy to modify and conjugate Difficult to modify
Production Synthesis, reduced manufacturing time and cost Expression, long and expensive in vivo manufacturing procedures

Aptamer Optimization

Since the discovery in 1990, thousands of aptamers have been identified with great potential for biomarker diagnosis, drug delivery, and disease therapies. However, only Macugen was approved by the Food and Drug Administration (FDA) for clinical use, and few of them have been employed in clinical assessment. The application of aptamers is limited due to their hydrophilic properties, high-affinity loss during production, and rapid excretion. Therefore, numbers of optimization approaches have been explored to improve the performance of aptamers, which mainly include but is not limited to:

  1. Aptamer basic sequences optimization
  2. Aptamer structure stabilization
  3. Aptamer hydrophobic/ hydrophilic portions optimization
  4. Chemical modifications
  5. Aptamer conjugations
  6. SELEX optimization
  7. Post-SELEX optimization

Some representative models of modified aptamers for disease diagnosis and therapy. Fig.1 Some representative models of modified aptamers for disease diagnosis and therapy. (Sun, 2015)

Aptamer Optimization Services at Creative Biolabs

Currently, numbers of therapeutic aptamers are evaluated in preclinical and clinical trials. In practice, however, the applications of aptamer, although sometimes successful, are usually much less efficient and successful than initially predicted.

As a pioneer and the undisputed global leader in novel drug discovery and manufacturing, Creative Biolabs has won a good reputation in providing support for aptamer development and optimization. Our professional scientists are confident in offering domestic and international customers a range of tailored strategies and services for the optimization of aptamers. All you need to do is contact us directly, and communicate with us about your specific demands or ideas. Our seasoned scientists will reply to you with a custom solution as soon as possible.

Reference

  1. Sun, H.G, Zu, Y.L. A Highlight of Recent Advances in Aptamer Technology and Its Application. Molecules. 2015, 20(7), 11959-11980.

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Questions & Answer

A: Creative Biolabs employs chemical modifications, such as backbone modifications, base modifications, and locked nucleic acids (LNAs), to enhance aptamer stability and resistance to nuclease degradation.

A: Aptamer optimization can benefit a wide range of applications, including but not limited to diagnostics, therapeutics, biosensors, targeted drug delivery, and imaging.

A: The timeline for aptamer optimization services can vary depending on the specific project requirements and the complexity of the target. Creative Biolabs provides project-specific timelines after assessing the project scope.

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