University of Toronto, Chemistry, 80 St. George Street, Toronto, Ontario M5S 3H6, Canada.
Nat Chem. 2011 Jun 23;3(7):509-24. doi: 10.1038/nchem.1062.
Peptide macrocycles have found applications that range from drug discovery to nanomaterials. These ring-shaped molecules have shown remarkable capacity for functional fine-tuning. Such capacity is enabled by the possibility of adjusting the peptide conformation using the techniques of chemical synthesis. Cyclic peptides have been difficult, and often impossible, to prepare using traditional synthetic methods. For macrocyclization to occur, the activated peptide must adopt an entropically disfavoured pre-cyclization conformation before forming the desired product. Here, we review recent solutions to some of the major challenges in this important area of contemporary synthesis.
肽大环化合物在药物发现到纳米材料等领域都有应用。这些环状分子在功能微调方面表现出了显著的能力。这种能力得益于使用化学合成技术来调整肽构象的可能性。使用传统的合成方法，环状肽的制备一直很困难，而且往往是不可能的。为了发生环化，在形成所需产物之前，活化的肽必须采用一种熵不利的预环化构象。在这里，我们综述了当前解决这一重要合成领域的一些主要挑战的方法。
