Purpose: The goal of this work was to develop a fast and accurate method to monitor PEGylation reactions by using HPLC with complementary UV/Vis and charged aerosol detection. It is an increasingly common practice to modify biotherapeutic peptides, proteins and small molecules by attaching chemical groups designed to enhance properties such as bioavailability, potency or stability. One example ...

The use of proteins as therapeutics has a long history and is becoming ever more common in modern medicine. While the number of protein-based drugs is growing every year, significant problems still remain with their use. Among these problems are rapid degradation and excretion from patients, thus requiring frequent dosing, which in turn increases the chances for an immunological response as wel...

The obstacles to the development of therapeutic aptamers for systemic inflammatory diseases, such as nuclease degradation and renal clearance, have not been fully overcome. Here, we report a novel PEGylation method, sbC-PEGylation, which improves the pharmacokinetic properties of RNA aptamers that act against interleukin-17A (IL-17A) in mice and monkeys. sbC-PEGylated aptamers were synthesized ...

In the process of finding better therapeutics, thousands new molecules are synthesised every day. Many these can be poorly soluble in water, leading to a potentially promising drug being rejected during testing due its poor solubility. Polyethylene glycol (PEG) has become known as an excellent modification remedy this and was initially used increase circulation time reduce immunogenicity therap...

The paper discusses general problems in using PEG for conjugation to high or low molecular weight molecules. Methods of binding PEG to different functional groups in macromolecules is reported together with their eventual limitations. Problems encountered in conjugation, such as the evaluation of the number of PEG chains bound, the localisation of the site of conjugation in polypeptides and the...

hirudin is an anticoagulant agent of the salivary glands of the medicinal leech. recombinant hirudin (r-hir) displays certain drawbacks including bleeding and immunogenicity. to solve these problems, cysteine-specific pegylation has been proposed as a successful technique. however, proper selection of the appropriate cysteine residue for substitution is a critical step. this study has, for the ...