Artículos de revistas
Carbohydrate PEGylation, an approach to improve pharmacological potency
Fecha
2014-06Registro en:
Giorgi, María Eugenia; Agusti, Rosalia; Muchnik, Rosa; Carbohydrate PEGylation, an approach to improve pharmacological potency; Beilstein-institut; Beilstein Journal Of Organic Chemistry; 10; 6-2014; 1344-1444
1860-5397
Autor
Giorgi, María Eugenia
Agusti, Rosalia
Muchnik, Rosa
Resumen
Conjugation with polyethylene glycol (PEG), known as PEGylation, has been widely used to improve the bioavailability of proteins and low molecular weight drugs. The covalent conjugation of PEG to the carbohydrate moiety of a protein has been mainly used to enhance the pharmacokinetic properties of the attached protein while yielding a more defined product. Thus, glycoPEGylation was successfully applied to the introduction of a PEGylated sialic acid to a preexisting or enzymatically linked glycan in a protein. Carbohydrates are now recognized as playing an important role in host–pathogen interactions in protozoal, bacterial and viral infections and are consequently candidates for chemotherapy. The short in vivo half-life of low molecular weight glycans hampered their use but methods for the covalent attachment of PEG have been less exploited. In this review, information on the preparation and application of PEG-carbohydrates, in particular multiarm PEGylation, is presented.