固相肽合成（SPPS），C端与侧链锚定：现实还是神话。

Solid-phase peptide synthesis (SPPS), C-terminal vs. side-chain anchoring: a reality or a myth.

作者信息

Cherkupally Prabhakar, Acosta Gerardo A, Ramesh Suhas, De la Torre Beatriz G, Govender Thavendran, Kruger Hendrik G, Albericio Fernando

机构信息

Catalysis and Peptide Research Unit, School of Health Sciences, University of Kwazulu-Natal, Durban, 4001, South Africa.

出版信息

Amino Acids. 2014 Aug;46(8):1827-38. doi: 10.1007/s00726-014-1746-7. Epub 2014 Apr 26.

DOI:10.1007/s00726-014-1746-7

PMID:24770904

Abstract

Here we review the strategies for the solid-phase synthesis of peptides starting from the side chain of the C-terminal amino acid. Furthermore, we provide experimental data to support that C-terminal and side-chain syntheses give similar results in terms of purity. However, the stability of the two bonds that anchor the peptide to the polymer may determine the overall yield and this should be considered for the large-scale production of peptides. In addition, resins/linkers which do not subject to side reactions can be preferred for some peptides.

摘要

在这里，我们回顾了从C端氨基酸侧链开始进行肽固相合成的策略。此外，我们提供实验数据以支持C端合成和侧链合成在纯度方面给出相似的结果。然而，将肽固定到聚合物上的两个键的稳定性可能决定总产率，并且在肽的大规模生产中应考虑这一点。另外，对于某些肽而言，不易发生副反应的树脂/连接体可能更受青睐。