Getting in Shape: Controlling Peptide Bioactivity and Bioavailability Using Conformational Constraints

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• 作者：Jonathan E. Bock ; Jason Gavenonis ; Joshua A. Kritzer
• 刊名：ACS Chemical Biology
• 出版年：2013
• 出版时间：March 15, 2013
• 年：2013
• 卷：8
• 期：3
• 页码：488-499
• 全文大小：435K
• 年卷期：v.8,no.3(March 15, 2013)
• ISSN：1554-8937

文摘

Chemical biologists commonly seek out correlations between the physicochemical properties of molecules and their behavior in biological systems. However, a new paradigm is emerging for peptides in which conformation is recognized as the primary determinant of bioactivity and bioavailability. This review highlights an emerging body of work that directly addresses how a peptide鈥檚 conformation controls its biological effects, cell penetration, and intestinal absorption. Based on this work, the dream of mimicking the potency and bioavailability of natural product peptides is getting closer to reality.