Protein epitope mimetics provide powerful tools to study biomolecular recognition in many areas of chemical biology. They may also provide access to new biologically active molecules and potentially to new classes of drug and vaccine candidates. Here we highlight approaches for the design of folded, structurally defined epitope mimetics, by incorporating backbone and side chains of hot residues onto a stable constrained scaffold. Using robust synthetic methods, the structural, biological, and physical properties of epitope mimetics can be optimized, by variation of both side chain and backbone chemistry. To illustrate the potential of protein epitope mimetics in medicinal chemistry and biotechnology, we present studies in two areas of infectology; the discovery of new antibiotics targeting essential outer membrane (OM) proteins in Gram-negative bacteria and the design of supramolecular synthetic vaccines.

中文翻译：

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蛋白质表位模拟物：从新型抗生素到超分子合成疫苗

蛋白质表位模拟物为研究化学生物学许多领域中的生物分子识别提供了强大的工具。它们还可能提供获取新的生物活性分子的途径，并可能提供获取新型药物和疫苗候选物的途径。在这里，我们通过将热残基的主链和侧链结合到稳定的受限支架上，重点介绍了折叠的，结构定义的表位模拟物的设计方法。使用可靠的合成方法，可以通过改变侧链和骨架化学来优化表位模拟物的结构，生物学和物理性质。为了说明蛋白质表位模拟物在药物化学和生物技术中的潜力，我们提出了两个感染学领域的研究。