论文部分内容阅读
骨架环肽是线性肽的C端和N端通过酰胺键进行首尾环合而形成的环状分子.研究者从细菌、真菌、植物和动物中发现了大量的骨架环肽.这种首尾环合的结构,使得骨架环肽具有很好的酶稳定性、热稳定性和化学稳定性,部分骨架环肽具有细胞膜通透性.骨架环肽分子异常的稳定性和高效的生物活性,使得其成为目前药物领域的研究热点.为了更深入地研究它们的结构和功能,骨架环肽的制备成为一个重要问题.概述了化学合成骨架环肽的一些方法,包括:(1)固相环合策略;(2)液相环合策略;(3)分子内自然化学连接策略,并对这些方法的特点和效率进行了讨论比较.
Cyclic cyclopeptides are cyclic molecules formed by the cyclization of the C-terminus and the N-terminus of a linear peptide through an amide bond. Researchers have discovered a large number of cyclic cyclopeptides from bacteria, fungi, plants and animals. , Which makes the cyclic cyclopeptide have good enzyme stability, thermal stability and chemical stability, and part of the cyclic cyclic peptide has cell membrane permeability.The unusual stability and efficient biological activity of the cyclic cyclic peptide make it become At present, there is a great research hotspot in the field of medicine.In order to study their structure and function in-depth, the preparation of scaffolds has become an important issue.Some methods of chemical synthesis of scaffolds are summarized, including: (1) (2) liquid-phase cyclization strategy, (3) intramolecular natural chemical linking strategy, and the characteristics and efficiency of these methods were discussed and compared.