Getting in shape: controlling peptide bioactivity and bioavailability using conformational constraints.
Getting in shape: controlling peptide bioactivity and bioavailability using conformational constraints.
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DOI：
10.1021/cb300515u
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发表时间：
2013-03-15
影响因子：
4
通讯作者：
Kritzer JA
中科院分区：
文献类型：
--
作者：
Bock JE;Gavenonis J;Kritzer JA
化学生物学家通常寻求分子的物理化学性质与其在生物系统中的行为之间的相关性。然而，一种新的模式正在出现的肽，其中构象被认为是生物活性和生物利用度的主要决定因素。这篇综述强调了一个新兴的工作机构，直接解决了肽的构象如何控制其生物学效应，细胞渗透和肠道吸收。基于这项工作，模仿天然产物肽的效力和生物利用度的梦想越来越接近现实。
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’s 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.