Automated incorporation of polyethylene glycol into synthetic oligonucleotides

̈schke, Andres Ja; ̈rste, Jens P. Fu; Cech, Dieter; Erdmann, Volker A.

doi:10.1016/s0040-4039(00)60572-5

Cited by 42 publications

(26 citation statements)

References 12 publications

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“…The method allows charge-specic graing of hydrophilic PEG molecules onto the DNA backbone, unlike previously reported chemical modication to obtain DNA-PEG conjugates. 21,[71][72][73][74] The noncovalent approach for PEGylation of oligonucleotides described here can potentially be considered as a third generation PEGylation approach in relation to the existing methods. 75,76 The process renders metal-free DNA molecules.…”

Section: Discussionmentioning

confidence: 99%

Electrostatically PEGylated DNA enables salt-free hybridization in water

et al. 2019

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Section: Discussionmentioning

confidence: 99%

Electrostatically PEGylated DNA enables salt-free hybridization in water

et al. 2019

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“…Jäschke et al have developed a suite of PEG-modified phosphoramidites and controlled pore glass (CPG) to incorporate PEG into 5′, 3′, or internal positions of ONs through automated DNA synthesis (Fig. 1(a)) [64, 65]. A large library of PEGylated ONs with different PEG M W (400 Da to 4 kDa) and conjugation sites has been successfully prepared.…”

Section: Pegylation Of Ons Using Linear or Slightly Branched Pegmentioning

confidence: 99%

PEGylation of therapeutic oligonucletides: From linear to highly branched PEG architectures

Zhang

2018

Nano Res.

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PEGylation, the attachment of poly(ethylene glycol) (PEG), has been adopted to improve the pharmacokinetic properties of oligonucleotide therapeutics for nearly 30 years. Prior efforts mainly focused on the investigation of linear or slightly branched PEG having different molecular weights, terminal functional groups, and possible oligonucleotide sites for functionalization. Recent studies on highly branched PEG (including brush, star, and micellar structures) indicate superior properties in several areas including cellular uptake, gene regulation efficacy, reduction of side effects, and biodistribution. This review focuses on comparing the effects of PEG architecture on the physiochemical and biological properties of the PEGylated oligonucleotide.

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“…One way to tackle these problems is to functionalize pharmaceutically active nucleic acids with PEG. [93] Direct coupling of PEG [90] or coupling through a linker molecule [91] has resulted in increased stability of oligonucleotides towards enzymatic degradation, prolonged plasma permanence, and enhanced penetration into cells by masking the negative charges of ODNs. One DBC drug already commercialized in 2004 is a PEGylated 28-mer aptamer, PEG-aptanib, which was approved by the FDA for the treatment of age-related macular degeneration of the retina.…”

Section: Biomedicinementioning

confidence: 99%