2016 lecture series 171st IBB Seminar Thioamide Probes for Studying Peptide Stability in vitro and in vivo 講師:Dr. E. James Petersson Associate Professor Department of Chemistry University of Pennsylvania 231 South 34th Street Philadelphia, PA 19104-6323, USA 日時:平成 28 年 3 月 3 日(木)14:00~16:00 会場:東京医科歯科大学 生体材料工学研究所 第一会議室 21 号館(3 階) Abstract: Our laboratory has demonstrated that thioamide substitutions of the peptide bond can be used as fluorescence quenchers to study protease activity, where thioamide placement allows one to observe cleavage at particular sites. During our investigations of protease sensor design, we have found that thioamide substitutions at the scissile bond can dramatically reduce cleavage of peptides by proteolysis. We have exploited this discovery to make versions of the signaling hormone GLP-1 that are stabilized by 1000-fold relative to native GLP-1, while retaining biological activity. Such stabilized peptides can be used as injectable therapeutics, and thioamides offer a facile way of making stable versions of newly discovered peptides for in vivo investigations. お問い合せ:生体材料工学研究所 メディシナルケミストリー分野 田辺(内線 6262) 、玉村
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