中文摘要：

二酮哌嗪类化合物（Diketopiperazines，DKPs）的特征结构是由两个氨基酸通过肽键缩合而成的环二肽（Cyclic dipeptides），稳定的六元环骨架结构使DKPs在药物化学中成为一个重要的药效团，表现出多种生物活性与药理活性，日益引起人们的极大关注。随着现代生物技术和高通量测序技术的飞速发展，人们对DKPs生物合成的分子机制与酶学机理的认识不断深入，DKPs中氨基酸缩合的分子机制主要有两种：非核糖体肽合成酶（Non-ribosomal peptide synthases，NRPSs）途径和环二肽合成酶（Cycliodipeptide synthases，CDPSs）途径。本文就近年来DKPs的生物合成相关研究进展进行了综述。

英文摘要：

Diketopiperazines （DKPs） are derivatives of cyclodipeptides resulted from the condensation of two amino acids. The conformationally constrained six-membered ring makes DKP an attractive pharmacophore in medicinal chemistry. Recently, there has been increasing interest in the natural DKPs due to their diverse bioactivities and pharmacological activities. Advances in modern biotechnologies and high throughput sequencing technologies have promoted our understanding of DKPs biosynthesis both on enzymatic and genetic levels. Biosynthesis of DKPs can be achieved either by non-ribosomal peptide synthases （NRPSs） or cycliodipeptide synthases （CDPSs）. This paper provides a brief overview of recent progresses on DKPs biosynthesis.