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Peptide Nucleic Acid PEGylation

Peptide Nucleic Acids (PNAs) are synthetic DNA mimics known for their exceptional binding strength and sequence specificity. While PNAs hold great promise in gene regulation and molecular diagnostics, their clinical application can be limited by poor water solubility and suboptimal pharmacokinetics. Our PNA PEGylation services are designed to overcome these limitations through precise, site-specific PEG conjugation. By attaching polyethylene glycol (PEG) chains to PNAs, we enhance their biostability, solubility, cellular uptake, and in vivo circulation time—making them more effective for use in drug delivery systems, nanomedicine platforms, and diagnostic assays.

What is Peptide Nucleic Acid PEGylation?

Peptide Nucleic Acid (PNA) is a synthetic analogue of DNA/RNA characterized by a peptide-like backbone structure, allowing it to bind to nucleic acids with high affinity and specificity. Polyethylene glycol (PEG) is a biocompatible and hydrophilic polymer often used to modify biomolecules. PEGylation is the process of covalently attaching PEG chains to molecules, including drugs, peptides, or proteins. PEGylation of PNAs refers to the chemical modification of peptide nucleic acids by covalently attaching PEG polymers to their backbone. PNAs are synthetic analogs of DNA or RNA with a unique peptide-like backbone, allowing for strong and selective hybridization with target nucleic acid sequences. PEG (polyethylene glycol), a highly hydrophilic and biocompatible polymer, is widely used to improve the pharmacological properties of therapeutic molecules.

Mechanism of Action

PEGylated PNA is created by chemically modifying PNA to introduce reactive groups (e.g., amines or thiols), which are then conjugated to PEG via esterification or amide bond formation. PEGylated PNA combines the high-affinity nucleic acid binding of peptide nucleic acid (PNA) with the stabilizing effects of polyethylene glycol (PEG). The PEGylation enhances PNA's solubility, reduces nonspecific adsorption, and prolongs circulation time, improving its efficacy in gene regulation.

The Importance of Peptide Nucleic Acid PEGylation

PEGylation significantly enhances the therapeutic potential of peptide nucleic acid (PNA) through multiple key benefits:

Enhanced Stability

The covalent attachment of polyethylene glycol (PEG) shields PNA from enzymatic degradation and improves its resistance to biological clearance, extending its shelf life and in vivo durability.

Improved Solubility

PEGylation increases PNA's hydrophilicity, preventing aggregation and ensuring better dispersion in aqueous solutions, facilitating easier formulation and administration.

Prolonged Circulation Time

The PEG corona reduces renal filtration and minimizes nonspecific interactions, significantly extending PNA's plasma half-life for sustained therapeutic effects.

Reduced Immunogenicity

PEG coating masks PNA from immune recognition, lowering the risk of adverse immune reactions and improving biocompatibility.

Targeted Delivery

PEGylated PNA can be further functionalized with ligands (e.g., antibodies, peptides) for tissue-specific delivery, enhancing precision in gene silencing or antisense therapy.

Collectively, these advantages make PEGylated PNA a versatile tool for therapeutics, diagnostics, and nanotechnology.

Guide to Peptide Nucleic Acid PEGylation Services

Custom PNA Synthesis and PEG Conjugation

PNA Oligonucleotide Synthesis

High-purity custom sequences (5–30mer)

Sequence design and modification support

PEG Type Selection

Linear PEGs (MW 500–20kDa)

Branched PEGs (2-arm, 4-arm)

Functional PEGs (NHS, Maleimide, Azide, Biotin, Fluorophore)

Site-Specific PEGylation Services

Terminal and Internal PEGylation

N-terminus, C-terminus, or internal lysine/cysteine residues

Chemistry Options

NHS ester – amine coupling

Maleimide – thiol conjugation

Click chemistry (azide–alkyne cycloaddition)

Multifunctional PEG Scaffolds

PNA–PEG–Drug, PNA–PEG–Antibody, PNA–PEG–Nanoparticle conjugates

Purification & Quality Control

Purification Techniques

Reverse-phase HPLC

Size-exclusion chromatography (SEC)

Analytical Characterization

Mass spectrometry (LC-MS or MALDI-TOF)

UV/Vis spectrophotometry

Degree of PEGylation confirmation

NMR analysis (upon request)

Advanced Functionalization (Optional)

Cell-Penetrating Enhancements

CPP addition for intracellular delivery

a Bioconjugation Capabilities

Antibody or aptamer targeting

siRNA, miRNA, or oligo hybrid design

Nanocarrier Integration

Liposome or gold nanoparticle PEGylated PNA complexes

Step-by-Step Workflow of Peptide Nucleic Acid PEGylation Service

1 Project Consultation

  • Client submits PNA sequence, PEGylation goals, and application context.
  • We provide feasibility assessment and chemistry recommendations.

2 PNA Synthesis

  • PNA is synthesized with high fidelity via solid-phase peptide synthesis (SPPS).
  • Optional: Functional group incorporation (e.g., amine, thiol, azide handles).

3 PEG Conjugation

  • PEG reagent selection based on desired MW, structure, and functionality.
  • Site-specific PEGylation using optimized conjugation chemistry.

4 Purification & QC Analysis

  • RP-HPLC and SEC purification to remove byproducts and free PEG.
  • Mass spectrometry and UV analysis for purity and PEGylation confirmation.

5 Final Delivery

  • Lyophilized or solution-phase PEGylated PNA delivered with:
  • Certificate of Analysis (CoA)
  • MS, HPLC chromatograms
  • Handling and storage guide

Key Benefits of Choosing Our Peptide Nucleic Acid PEGylation Services

Custom-Tailored Conjugation Strategies

We offer flexible PEGylation strategies tailored to your sequence, application, and functional group needs.

High-Purity PNA-PEG Products

All products undergo rigorous HPLC purification and LC-MS analysis to ensure batch-to-batch consistency and high purity.

Scalable for Research to Preclinical Use

From μmol-scale discovery batches to multi-mg preclinical lots—we adapt to your stage of development.

Enhanced Stability and Bioavailability

PEGylated PNAs demonstrate improved resistance to enzymatic degradation and increased plasma half-life.

Wide PEG Chemistry Portfolio

Access to linear, branched, heterobifunctional, and multi-arm PEG reagents for full application flexibility.

Comprehensive Documentation & Support

Complete QC reports, storage recommendations, and technical support provided throughout the project.

Diverse Applications of PNA PEGylation

PEGylated PNA holds significant promise across multiple biomedical fields. These versatile applications highlight PEGylated PNA's potential in advancing precision medicine and biotechnology.

Drug Delivery

PNA PEGylation serves as a targeted carrier, enhancing therapeutic precision while minimizing off-target effects.

Gene Therapy

PEGylation improves PNA's cellular uptake and stability, enabling efficient gene modulation.

Diagnostic Tool

PEGylated PNA enables sensitive detection of genetic mutations and molecular imaging.

Biomaterials

Its incorporation into biomaterials enhances biocompatibility and biodegradability for tissue engineering and biosensors.

FAQs

FAQs about sgRNA Services

References

  1. PNA conjugated to high-molecular weight poly(ethylene glycol): synthesis and properties. PMID: 18066875 DOI: 10.1080/15257770701490548
  2. Inchworm-type PNA-PEG conjugate regulates gene expression based on single nucleotide recognition. PMID: 33798568 DOI: 10.1016/j.ijbiomac.2021.03.140
  3. PNA-PEG Modified Silicon Platforms as Functional Bio-Interfaces for Applications in DNA Microarrays and Biosensors. https://pubs.acs.org/doi/10.1021/bm801406w
  4. Suppression of Intracellular Gene Expression by Inchworm-Type PNA-PEG Conjugate Depends on Recognition of a Monobasic Mutation. https://doi.org/10.1246/bcsj.20210126
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