Randev, Rajan, Sayers, Claire, Ryan, Sinead, Mantovani, G. (Giuseppe), Keiper, Odin, Blindauer, Claudia A., Brayden, David J. and Haddleton, David M. (2008) POLY 433-site-specific conjugation of a well-defined functional poly(mPEG1100) methacrylate to salmon calcitonin : design, synthesis, characterization and investigation via NMR. In: 236th National Meeting of the American-Chemical-Society, Philadelphia, PA, 17-21 Aug 2008. Published in: Abstracts of papers of the American Chemical Society, Vol.236 433-POLY.

Abstract

The therapeutic value and nature of bio-molecules has been identified and exploited in numerous ways for several years. Conjugation of bio-molecules with synthetic molecules/macromolecules is one method of extending their lifetime by inhibiting degradation and excretion from the body to enhance therapeutic activity. One such technique is ‘pegylation' a term which refers to the combination of functionalized poly(ethylene glycol) with an appropriate bio-molecule. Commercially available, PEGylated drugs are in some cases a mixture of different positional isomers, the development of further generations of polymer therapeutic requires the design of site-specific conjugation strategies. Knowledge of the site of attachment will ensure both conjugation reproducibility and a better understanding of the bioconjugate structure/activity relationship. In this present work, the possibility of employing such end functional macromolecules for the targeting of the N-terminus of a biologically relevant peptide, salmon calcitonin was explored. The resultant polymer bio-conjugate was investigated by NMR and biological assays.

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