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Pegylacja - metoda zmiany właściwości leków polipeptydowych, substancji biologicznie aktywnych

Ferenc J., Kieć-Kononowicz K.

Wiadomości Chemiczne

2005

[Z] 59, 11-12

953--979

This review attempts to briefly summarize the recent developments in the area of PEGylation. Pegylation, the process by which polyethylene glycol chains are attached to as well protein and peptide drugs as low molecular weight molecules is used to modify the properties of drugs, biologically active structures. It has influence on pharmacokinetic and pharmacodynamic properties, stability and immunogenicity of structures. The advantages and drawbacks of such modifications were discussed. Pegylation of polypeptide and protein structures as well as small molecules was presented. Pegylation process was divided in two groups: pegylation of the first and second generation. Both processes were presented. Examples of pegylated drugs (Adagen, Oncaspar - first generation; PEG-intron, Pegasys, Somavert, Neulasta - second generation) already introduced into the market were shortly presented, structures being under investigation were mentioned.

Structure and activity studies of glycine receptor ligands : Part 4. N-[(7-arylalkyl, 7-aryloxyalkyl)-8-theophyllyl]-glycines

Drabczyńska A., Karolak-Wojciechowska J., Kieć-Kononowicz K.

Polish Journal of Chemistry

1999

vol. 73 nr 5

783-792

Preparation of N-[(7-arylalkyl, 7-aryloxyalkyl)-8-theophyllyl]-glycines by condensation of 8-bromo-theophylline with arylalkyl- and aryloxyalkylbromides and aminolysis with glycine is described. The structure of one of the obtained glycine derivatives was confirmed by X-ray analysis. A comparison of the glycine receptor binding model (molecule L-689,560) and the 3-D structure of that molecule indicates serious differences in molecule shape, explaining their inactivity.