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Related Experiment Video

Updated: Sep 20, 2025

Solid Phase Synthesis of a Functionalized Bis-Peptide Using "Safety Catch" Methodology
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Efficient synthesis of artificial pharmaceutical solid-phase modules for constructing aptamer-drug conjugates.

Fei Gao1, Hongli Huang2, Chunquan Sheng3

  • 1Institute of Translation Medicine, Shanghai University, Shanghai 200444, China.

Bioorganic Chemistry
|June 6, 2022
PubMed
Summary

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Researchers developed a novel method for creating aptamer-drug conjugates (ApDCs) using solid-phase synthesis. This approach simplifies the production of these targeted drug delivery systems, enhancing their potential for cancer therapy.

Area of Science:

  • Biotechnology
  • Pharmaceutical Sciences
  • Medicinal Chemistry

Background:

  • Aptamer-drug conjugates (ApDCs) are advanced targeted drug delivery systems designed to enhance therapeutic efficacy and minimize drug toxicity by specifically binding to molecular targets.
  • Existing ApDC strategies face challenges including complex synthesis, high costs, and poor control over drug binding sites and loading ratios.

Purpose of the Study:

  • To develop a simplified and efficient method for synthesizing aptamer-drug conjugates (ApDCs).
  • To overcome the limitations of current ApDC production, such as complicated synthesis, high cost, and lack of control over drug conjugation.

Main Methods:

  • Designed and synthesized an artificial pharmaceutical solid-phase module incorporating Combretastatin A-4 (CA-4) with an inactive ingredient as a bonding moiety.
Keywords:
Antitumor activityAptamersCombretastatin A-4ConjugateSolid-phase modules

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  • Utilized solid-phase synthesis technology for automated and efficient conjugation of the CA-4 module to aptamers at predetermined positions.
  • Conducted biological studies to evaluate the properties of the synthesized ApDCs.

    • Main Results:

    • Successfully synthesized novel ApDCs using the developed solid-phase module and synthesis technology.
    • The resulting ApDCs demonstrated maintained specific recognition capabilities for their targets.
    • Biological evaluation confirmed the definite cytotoxicity of these ApDCs against tumor cells.

    Conclusions:

    • The developed solid-phase synthesis approach offers an efficient and controllable method for producing aptamer-drug conjugates (ApDCs).
    • This strategy addresses key limitations of existing ApDC synthesis, paving the way for improved targeted cancer therapies.
    • The synthesized ApDCs show promise as effective therapeutic agents due to their specific targeting and potent cytotoxicity.