Site-defined peptide–antisense oligonucleotide conjugates with development-aware purification and analytics.
Chemically defined constructs designed to support uptake, targeting, and intracellular delivery for antisense workflows across modified DNA/RNA, PS gapmers, and high-affinity bases (LNA/BNA).
Peptide–ASO conjugation is the site-defined covalent attachment of a peptide to an antisense oligonucleotide (ASO) to create a chemically defined construct. This approach is designed to support cellular uptake, tissue targeting, and intracellular delivery while maintaining ASO integrity and functional antisense activity.
Peptide–ASO conjugates are also referred to as ASO–peptide conjugates or peptide–oligonucleotide conjugates, depending on orientation and application context.
Related services: Peptide Modifications, Peptide Bioconjugation, Click Chemistry Peptides, Cleavable Linker Peptides.
In contrast to lipid nanoparticle (LNP) formulations, peptide–ASO conjugates offer a chemically defined, single-component construct that simplifies characterization, reproducibility, and early-stage development workflows.
Common antisense formats, including mixed DNA/RNA designs, can be supported with appropriate handles and linkers.
Widely used for RNase H mechanisms; conjugation strategy is selected to preserve intended function.
Supports conformationally constrained bases that improve binding affinity and stability.
Conjugation feasibility depends on the available functional handle (e.g., thiol, amine, azide/alkyne) and the desired linker strategy. If you’re unsure, send the ASO design and constraints—we’ll recommend a practical handle + linker plan.
In addition to direct peptide–ASO conjugation, Bio-Synthesis can introduce lipid motifs as an ASO modification prior to peptide attachment to support dual-modality designs (lipid + peptide).
Lipid modification may be used to tune circulation behavior, protein binding, or membrane interaction prior to peptide delivery.
A common default for chemoselectivity and reproducible conversion.
Fast coupling using terminal thiols and maleimide handles.
Activated ester routes when click handles are constrained.
Selected when intracellular release is required (project-dependent).
Preferred when stable linkage is the priority.
Reaction conditions and workup are selected to minimize oligonucleotide degradation and preserve construct homogeneity.
This workflow supports feasibility studies through translational programs by aligning chemistry, purification, and analytics to the stage of development.
Bio-Synthesis can align conjugation strategy, purification, and analytical depth to the intended stage of development.
Analytical depth and documentation can be aligned to feasibility, preclinical, or translational workflows.
We support common antisense formats including modified DNA/RNA and PS gapmer designs, as well as high-affinity bases such as LNA and BNA. Feasibility depends on handle placement and linker strategy.
Yes. We can introduce lipid motifs as an ASO modification prior to peptide attachment to support dual-modality (lipid + peptide) constructs when appropriate.
Copper-free click is a common default for RNA compatibility and site specificity. Thiol–maleimide or amide coupling may be suitable depending on available handles. Cleavable or non-cleavable linkers can be selected based on stability and release requirements.
Send ASO sequence and modification pattern (DNA/RNA/PS/LNA/BNA), any lipid modification request, peptide sequence and handle/attachment preference, preferred linker chemistry (or ask us to recommend), plus target quantity and purity.
For the fastest quote, send your ASO sequence and modification pattern (DNA/RNA/PS/LNA/BNA), any lipid modification request, peptide sequence/handle, preferred attachment site (or constraints), linker preference (or “recommend”), and quantity/purity targets.
Not sure which route is safest? Send sequences and constraints—we’ll propose a handle + linker plan aligned to your ASO chemistry.
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