【摘 要】
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An increasing number ofpeptides/proteins are being developed as therapeutic agents.However,peptides/proteins are generally much less stable than small molecule drugs.Their instability behavior greatly
【出 处】
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2008中国深圳蛋白质和多肽科学大会
论文部分内容阅读
An increasing number ofpeptides/proteins are being developed as therapeutic agents.However,peptides/proteins are generally much less stable than small molecule drugs.Their instability behavior greatly limits the choice and preparation of such drug delivery systems,presenting unique challenges.In this presentation,a model peptide (31 aa) is shown to be unstable not only in an aqueous environment but also in several organic solvents.It was found that the major degradation pathway is dimerization in organic solvents,initiated through an intramolecular deamidation/dehydration step,followed by intermoleeular nucleophilic attack.Based on the degradation mechanisms,two strategies were designed-(1) acidification of the peptide at low temperature and (2) addition of a key chelating metal in the system.Both strategies were found to be very effective in overcoming thestability challenges.
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