Department of Chemistry, University of Rochester, Rochester, New York 14627, USA.
J Org Chem. 2013 Apr 19;78(8):3525-31. doi: 10.1021/jo400119s. Epub 2013 Mar 29.
Macrocyclic peptides have emerged as attractive molecular scaffolds for the development of chemical probes and therapeutics. In this synopsis, we highlight contemporary strategies to access peptide macrocycles from ribosomally produced polypeptides. Challenges that have been tackled in this area involve orchestrating the desired macrocyclization process in the presence of unprotected polypeptide precursors and expanding the functional space encompassed by these molecules beyond that of canonical amino acid structures. Applications of these methodologies for the discovery of bioactive molecules are also discussed.
大环肽已成为开发化学探针和治疗药物的有吸引力的分子支架。在这篇综述中，我们重点介绍了从核糖体产生的多肽中获得肽大环的当代策略。在这个领域中，已经解决了一些挑战，包括在未保护的多肽前体存在的情况下，协调所需的大环化过程，并将这些分子的功能空间扩展到经典氨基酸结构之外。还讨论了这些方法在发现生物活性分子方面的应用。
