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Strategies for Fine-Tuning the Conformations of Cyclic Peptides.
Chemical Reviews ( IF 51.4 ) Pub Date : 2020-08-05 , DOI: 10.1021/acs.chemrev.0c00013
Rasha Jwad 1 , Daniel Weissberger 2 , Luke Hunter 2
Affiliation  

Cyclic peptides are promising scaffolds for drug development, attributable in part to their increased conformational order compared to linear peptides. However, when optimizing the target-binding or pharmacokinetic properties of cyclic peptides, it is frequently necessary to “fine-tune” their conformations, e.g., by imposing greater rigidity, by subtly altering certain side chain vectors, or by adjusting the global shape of the macrocycle. This review systematically examines the various types of structural modifications that can be made to cyclic peptides in order to achieve such conformational control.

中文翻译:

精细调整环肽构象的策略。

环肽是用于药物开发的有前途的支架,部分归因于与线性肽相比,其构象顺序增加。但是,当优化环肽的靶点结合或药代动力学特性时,通常有必要“微调”其构象,例如,通过施加更大的刚性,巧妙地改变某些侧链载体或通过调节环的整体形状来“微调”它们的构象。大循环。这篇综述系统地检查了可以对环肽进行的各种类型的结构修饰,以实现这种构象控制。
更新日期:2020-09-10
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