Inside Cover: General and Facile Route to Isomerically Pure Tricyclic Peptides Based on Templated Tandem CLIPS/CuAAC Cyclizations (Angew. Chem. Int. Ed. 2/2018),Angewandte Chemie International Edition

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Inside Cover: General and Facile Route to Isomerically Pure Tricyclic Peptides Based on Templated Tandem CLIPS/CuAAC Cyclizations (Angew. Chem. Int. Ed. 2/2018)
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2017-12-18 , DOI: 10.1002/anie.201712562
Gaston J. J. Richelle ₁ , Sumeet Ori ₁ , Henk Hiemstra ₁ , Jan H. van Maarseveen ₁ , Peter Timmerman ₂

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A scaffold-assisted one-pot CLIPS/CuAAC ligation/multicyclization reaction based on the use of flexible tetravalent scaffolds enables the conversion of linear peptides into single-isomeric tricyclic peptides. In their Communication on page 501 ff., J. H. van Maarseveen, P. Timmerman et al. show that there are no practical limitations to the nature and amount of amino acids present in the loops. This method can be used for the high-throughput synthesis of tricyclic peptides followed by subsequent screenings for the identification of potent peptide therapeutics.

中文翻译：

封面内容：基于模板化串联CLIPS / CuAAC环化的异构纯三环肽的通用且简便途径（Angew。Chem。Int。Ed。2/2018）

基于使用柔性四价支架的支架辅助一锅式CLIPS / CuAAC连接/多环化反应可将线性肽转化为单异构三环肽。J. H. van Maarseveen，P. Timmerman等人在其第501页及以下的通讯中。证明环中存在的氨基酸的性质和数量没有实际限制。该方法可用于三环肽的高通量合成，然后进行后续筛选以鉴定有效的肽治疗剂。

更新日期：2018-01-04

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