BOC Sciences is a leading supplier of PEGylation reagents, with a full range of PEG derivatives, including: NHS-PEG, maleimide PEG, thiol PEG, amino PEG, azide PEG, DSPE PEG, fluorescent PEG, etc. Our team of experts has extensive experience in the development & optimization of PEG oligonucleotide conjugates , ensuring that our customers receive high-quality PEGylated oligonucleotides.
Fig.1 PEG-conjugated oligonucleotide synthesis. (Chowdhury et al., 2023)
PEG conjugated oligonucleotide refers to the covalent attachment of polyethylene glycol (PEG) to an oligonucleotide molecule, which significantly improves the pharmacokinetic properties of the target molecule, and has a wide range of applications in gene therapy.
Oligonucleotide drugs include DNA, CpGDNA, and interfering RNA, which have been widely proven to have gene knockout, improve immunity, and treat tumors. However, due to the short half-life of the oligonucleotide drugs in the body, the structure is susceptible to damage by various enzymes, which reduces the drug efficacy, thereby limiting its clinical use. PEG modification can solve the problem of such drugs. In the study of antisense DNA, it was found that the in vivo half-life of antisense DNA modified by PEG with a phosphorothioate bond as the backbone (PSODN) is extended, which is ten times that of ordinary PSODN. PEG can form a three-dimensional protective film in water, wrapped around the surface of nucleoside drugs, shielding the surface negative charges, which is beneficial for the uptake of nucleoside drugs by the corresponding cells and improves the effect.
(1) Enhanced solubility. PEG has excellent solubility properties and can significantly increase the solubility of oligonucleotides in aqueous solution;
(2) Enhanced resistance to enzymatic degradation. Oligonucleotides are susceptible to nuclease degradation in living organisms, while PEG modification can form a protective layer and reduce enzyme recognition and degradation, thus prolonging the half-life of oligonucleotides;
(3) Reduced immunogenicity. PEG has low immunogenicity and can reduce the interaction of oligonucleotides with the immune system;
(4) Improved biodistribution. By PEG modification, the circulation time of oligonucleotides in the blood can be increased, and clearance by the liver and kidney can be reduced, thus increasing the accumulation of oligonucleotides in the target tissue or organ;
BOC Sciences offers a comprehensive range of bioconjugation services to meet the specific needs of researchers and pharmaceutical companies. Our expertise in oligonucleotide synthesis and PEG conjugation enables us to provide high-quality custom synthesis, purification, and characterization services.
PEG conjugated oligonucleotide can be used as an effective vector to deliver modified nucleic acid sequences for gene silencing, expression, or repair. PEG modification enhances the therapeutic potential of oligonucleotides by increasing stability, prolonging cycling time, and improving cellular uptake.
Through specific recognition of nucleic acid sequences, PEG conjugated oligonucleotides can inhibit viral replication or bacterial growth by targeting essential genetic elements.
By incorporating PEG modifications, oligonucleotide probes can exhibit improved hybridization efficiency, specificity and resistance to nuclease degradation. These properties make them valuable tools for a variety of diagnostic techniques, including polymerase chain reaction (PCR), fluorescence in situ hybridization (FISH) and microarray-based assays.
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PEG conjugation to oligonucleotides typically involves the covalent attachment of a PEG molecule to the oligonucleotide's functional groups. This process can be achieved through chemical cross-linking or other conjugation methods like NHS or maleimide chemistry, depending on the PEG derivative used. The result is a stable PEGylated oligonucleotide ready for various applications.
BOC Sciences offers a variety of PEG derivatives for oligonucleotide conjugation, including NHS-PEG, maleimide PEG, thiol PEG, and amino PEG. Each derivative serves different conjugation needs, allowing for flexibility in modifying oligonucleotides for specific applications, such as improving solubility or enabling targeted delivery.
PEGylated oligonucleotides exhibit enhanced resistance to nuclease degradation, which improves their performance in hybridization assays. The PEG modification protects the oligonucleotide from enzymatic breakdown, allowing for more reliable and consistent results in techniques like PCR, FISH, or microarray assays.
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