Oligonucleotide-peptide Conjugation

Oligonucleotide-peptide conjugates always exhibit a strong biological effect in a variety of applications, and they can be used to improve both cellular specificity and intracellular delivery of antisense or antigene compounds or to modify functions of the peptide or protein. As a service provider in bioconjugation, we have successfully accomplished numerous challenging oligonucleotide conjugation projects. Now, Creative Biolabs can offer high-quality oligonucleotide-peptide conjugation services by using the raw materials containing synthetic oligonucleotide and peptide provided by our customers all over the world.

Oligonucleotide-peptide Conjugation at Creative Biolabs

Oligonucleotide-peptide conjugates are chimeric molecules composed of synthesized oligonucleotide (DNA or RNA) linked to the peptide. Oligonucleotide-peptide chemical conjugation can add some biological and biophysical properties of peptides to oligonucleotides. Up to now, a considerable number of different conjugates possibilities have been developed and investigated extensively. Creative Biolabs provides a wide variety of oligonucleotide synthesis scales, modifications, conjugations, and purifications to customize your oligonucleotide-peptide conjugates to meet exacting requirements.

• Conjugation Methods

  Several distinct synthetic approaches (either stable or cleavable linkages) have been developed for the conjugation of peptides to the oligonucleotides. In the stepwise solid-phase synthesis approach, the oligonucleotide and peptide is usually assembly by using respective automated solid-phase synthesis on the same solid supports. However, conjugation of these functionalized molecules is often limited by the side-reactions resulting in the noncompatible standard syntheses of the two components. To overcome such difficulty, Creative Biolabs applies post-synthetic conjugation approaches for the chemical synthesis of oligonucleotide-peptide conjugates. This strategy allows that the peptides and oligonucleotides are post-synthetic conjugations using the most appropriate formation of several linkages such as the oxime, amide bonds, carbonyl linkages, thioether formation, disulfide linkages, click chemistry and others.

Figure 1. Preparation of oligonucleotide-peptide conjugates. (Aviñó, 2011)

• Conjugation Sites

  A variety of different conjugation sites are available selections in oligonucleotide-peptide conjugation. The N- or C-terminus of peptides have frequently been used to conjugate at the 5'- and/or 3'- terminus ends of the oligonucleotide because of easy chemical conjugation and minimal interference with oligonucleotides base pairing. Besides, the 2'-positions of a ribose sugar, nucleobases at the internal positions, and internucleotide phosphodiester bonds could also be used for conjugation.

Figure 2. The intracellular delivery of oligonucleotide conjugates. (Juliano, 2012)

Applications of Oligonucleotide-peptide Conjugation

These oligonucleotide-peptide conjugates are used in a variety of potential biological applications, which in fields ranging from therapeutics to nanotechnology. One of the most frequently and increasingly important applications of such chemical conjugation is to improve the cellular delivery of antisense or antigene compounds and therapeutic potential of these agents, where the peptide acts as an exceptionally versatile carrier. Oligonucleotides have been successfully attached to many peptides to enhance the cellular membrane permeability and study the molecular requirements for enzyme activity. Moreover, oligonucleotide-peptide conjugation is also used to allow the spatial immobilization of conjugates on DNA arrays or to modify peptide functions with oligonucleotide as regulatory elements. In addition, oligonucleotide-peptide conjugates have been served as the possible molecular tools (e.g., epitope mapping) and used as the testing tool in several sensing systems.

Figure 3. The potential sites available for the attachment of peptides. (Aviñó, 2011)

• Custom Mitochondrial Targeting Oligo Synthesis
  Mitochondrial-targeting oligos are designed to specifically target mitochondria within cells. They are used in illness therapy, gene regulation, and cellular metabolism research.

Features of Our Service

• A variety of oligonucleotides are available (DNA, RNA, siRNA, BNA)
• Solid-phase or solution-phase synthesis and conjugation
• Enable sequence terminal/internal conjugation
• Allow control of the spatial arrangement of the peptides
• Wide variety of synthesis approaches, modifications, treatments, and purifications
• Stringent quality control standards
• Fully traceable conjugation reports

Creative Biolabs is a leading service provider that tailors the best-fit proposal for oligonucleotide-peptide conjugation to meet your expected objectives. If you are interested in learning more about our capacity for oligonucleotide conjugation, please do not hesitate to contact us.

References

1. Aviñó, A.; et al. (2011). Synthesis of Oligonucleotide-Peptide Conjugates for Biomedical and Technological Applications. Bioconjugation Protocols. 223-238.
2. Juliano, R, L.; et al. (2012). The chemistry and biology of oligonucleotide conjugates. Accounts of Chemical Research. 45(7): 1067-1076.