CD Formulation's services in developing Peptide-ASO Conjugates aim to assist researchers and organizations in crafting versatile biomolecules. By merging peptides with antisense oligonucleotides, this tech expands the horizon for scientific inquiry and novel implementations.
The creation of peptide-ASO conjugates focuses on leveraging the benefits of peptides and ASOs to improve precision in targeting and efficiency in cellular delivery. This involves chemically joining these two components to capitalize on peptides' targeting abilities and ASOs' gene regulation capability, thus improving their effectiveness in reaching specific targets. Early research focused on optimizing conjugation methods and ensuring stability to address challenges related to membrane penetration and specific recognition.
In crafting peptide-ASO Complexes, peptides and oligos are automatically synthesized on solid supports. This enables the formation of robust links after synthesis using diverse chemical reactions such as oxime, amide, carbonyl, thioether, disulfide bonds, and click techniques. This flexible coupling method not only increases the success rate of synthesis but also enhances the functional properties of the final conjugate, laying a foundation for future applications.
When forming peptide-ASO conjugates, the peptide's N- or C-terminus often connects to the oligonucleotide's 5' or 3' end. This strategy aids in chemical linkage without significantly affecting base pairing. Beyond terminal sites, the 2' position of ribose, internal nucleobases, and the phosphodiester bond between nucleotides can also serve as effective binding sites. This variety in binding options provides flexibility in optimizing the performance of the conjugate, ensuring the final product's functionality and stability.
Fig.1 Flow chart of peptide-ASO conjugate development. (CD Formulation)
Define the project's goals, design the appropriate peptide-ASO conjugate structure, and select suitable peptide segments and oligonucleotides.
Individually synthesize peptides and oligonucleotides, and perform necessary chemical modifications to optimize their performance.
Connect peptides and oligonucleotides by selecting suitable chemical bonds (such as oxime or amide bonds) to ensure the stability of the conjugation.
Conduct tests on the peptide-ASO conjugates for stability, affinity, and cellular uptake to assess overall performance.
Implement strict quality control to ensure each conjugate meets the standards, and compile relevant documentation for client reference.
Items | Descriptions |
---|---|
HPLC Platform | HPLC is employed to separate and analyze the purity and composition of Peptide-ASO Conjugates, ensuring the quality of synthesized products. |
MS Platform | MS technology confirms the molecular structure and molecular weight of Peptide-ASO conjugates by measuring the mass-to-charge ratio of ions. |
CD Platform | CD is used to study the secondary structure of Peptide-ASO Conjugates, revealing their conformational characteristics. |
DLS Platform | DLS measures the size distribution of particles to assess the aggregation state and stability of Peptide-ASO Conjugates. |
Technology: Synthesis of peptide-oligonucleotide conjugates by chemical synthesis technology
Journal: Molecules
IF: 4.06
Published: 2021
Results:
The utilization of peptide-oligonucleotide conjugates (POCs) is gaining traction despite their high costs, as they significantly enhance cellular uptake and tissue delivery of nucleic acids like antisense oligonucleotides and siRNAs. This overview focuses on the chemical synthesis of POCs within the broader landscape of nucleic acid therapeutics, addressing the challenges of delivery, types of cell-penetrating peptides, intracellular transport mechanisms, and various applications including both non-covalent complex formation and covalent linking with oligonucleotides.
Fig.2 Synthesis of peptide-oligonucleotide conjugates (POCs). (Klabenkova K, et al., 2021)
CD Formulation is dedicated to providing clients with high-quality Peptide-ASO Conjugates development services. Please feel free to contact us for more information about our services.
References