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Basic Design Elements for Tunable Cation Transport Using Picolinic‐Acid‐Incorporated Tetrapeptides
ChemistrySelect ( IF 2.1 ) Pub Date : 2018-09-06 , DOI: 10.1002/slct.201801612
Debajyoti Basak 1 , Parichita Saha 2 , Nandita Madhavan 2
Affiliation  

Selective transport of cations across cell membranes is essential for various biological functions in the body. Synthetic pores that mimic the selectivity of natural ion channels are attractive for development of drugs and materials. Peptides are now emerging as attractive therapeutic agents due to their biocompatibility and ready accessibility. Herein, we report a systematic study that identifies key elements to design cation‐selective channels using tetrapeptide scaffolds. The scaffolds are derived from picolinic acid and alanine. Their ion transport activity is enhanced by hydrophobic long alkyl chains at the N‐terminus. These scaffolds are exciting as cation‐selectivity can be induced as well as switched by varying the oligoether groups at the C‐terminus.

中文翻译:

使用吡啶甲酸-酸性掺入的四肽进行阳离子运输的基本设计要素

阳离子跨细胞膜的选择性转运对于体内各种生物功能至关重要。模仿天然离子通道选择性的合成孔对于药物和材料的开发具有吸引力。肽由于其生物相容性和容易获得的特性,现在正成为有吸引力的治疗剂。在此,我们报告了一项系统研究,该研究确定了使用四肽支架设计阳离子选择性通道的关键要素。支架衍生自吡啶甲酸和丙氨酸。N端的疏水长烷基链增强了它们的离子迁移活性。这些支架令人兴奋,因为可以通过改变C端的寡醚基来诱导和转换阳离子选择性。
更新日期:2018-09-06
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