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抗衡离子在肽中的作用——概述

The Role of Counter-Ions in Peptides-An Overview.

作者信息

Sikora Karol, Jaśkiewicz Maciej, Neubauer Damian, Migoń Dorian, Kamysz Wojciech

机构信息

Department of Inorganic Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, 80-210 Gdańsk, Poland.

出版信息

Pharmaceuticals (Basel). 2020 Dec 3;13(12):442. doi: 10.3390/ph13120442.

Abstract

Peptides and proteins constitute a large group of molecules that play multiple functions in living organisms. In conjunction with their important role in biological processes and advances in chemical approaches of synthesis, the interest in peptide-based drugs is still growing. As the side chains of amino acids can be basic, acidic, or neutral, the peptide drugs often occur in the form of salts with different counter-ions. This review focuses on the role of counter-ions in peptides. To date, over 60 peptide-based drugs have been approved by the FDA. Based on their area of application, biological activity, and results of preliminary tests they are characterized by different counter-ions. Moreover, the impact of counter-ions on structure, physicochemical properties, and drug formulation is analyzed. Additionally, the application of salts as mobile phase additives in chromatographic analyses and analytical techniques is highlighted.

摘要

肽和蛋白质构成了一大类在生物体内发挥多种功能的分子。鉴于它们在生物过程中的重要作用以及化学合成方法的进展,对基于肽的药物的兴趣仍在不断增长。由于氨基酸的侧链可以是碱性、酸性或中性的,肽类药物通常以带有不同抗衡离子的盐的形式存在。本综述重点关注抗衡离子在肽中的作用。迄今为止,已有60多种基于肽的药物获得了美国食品药品监督管理局(FDA)的批准。根据它们的应用领域、生物活性以及初步测试结果,它们具有不同的抗衡离子。此外,还分析了抗衡离子对结构、物理化学性质和药物制剂的影响。此外,还强调了盐作为流动相添加剂在色谱分析和分析技术中的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c42f/7761850/edaa00e47b88/pharmaceuticals-13-00442-g002a.jpg

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