Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800, Kgs. Lyngby, Denmark.
Biopolymers. 2011;96(5):561-6. doi: 10.1002/bip.21571.
The field of peptoid (i.e., N-alkylglycine) research has been thriving since the first publications on this molecular design appeared in 1992. A highly efficient and modular synthetic platform, which is compatible with automation and ready generation of combinatorial libraries, was published the same year. This has enabled the investigation of numerous compounds with this architecture, and ligands with a wide variety of interesting biological targets have thus been discovered. Furthermore, detailed biophysical and structural studies focusing on the investigation of the conformational space adopted and three-dimensional folding of these peptide mimics have been undertaken. The same is true for beta-peptides (i.e., oligomers composed of beta-amino acids). Since the first publication describing peptide mimics combining these two structural modifications [the N-alkyl-beta-alanines (beta-peptoids)] in 1998, on the other hand, the application of this backbone construct has appeared much more sparsely in the literature. The present perspective article will provide an overview of the data obtained for beta-peptoid-containing peptide mimics as well as a discussion of the future challenges associated with this type of backbone modification.
自 1992 年首次发表关于这种分子设计的论文以来，肽（即 N-烷基甘氨酸）研究领域一直蓬勃发展。同年还发表了一个高效且模块化的合成平台，与自动化兼容，并可随时生成组合文库。这使得对这种结构的许多化合物以及具有各种有趣生物靶标的配体进行了研究。此外，还进行了详细的生物物理和结构研究，重点研究这些肽模拟物采用的构象空间和三维折叠。β-肽（即由β-氨基酸组成的寡聚物）也是如此。另一方面，自 1998 年首次发表描述将这两种结构修饰（N-烷基-β-丙氨酸（β-肽））结合在一起的肽模拟物的第一篇论文以来，这种骨架结构在文献中的应用要稀疏得多。本文将概述有关含β-肽的肽模拟物的研究数据，并讨论与这种类型的骨架修饰相关的未来挑战。
