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.
Highlights
Peptides along with proteins constitute the largest group of mediators of cellular processes making them pivotal for the functioning of many organisms
That the breakthrough of peptide synthesis dates back to the 1960s, peptides are still considered as poor drug candidates, mostly because of their poor bioavailability and the tendency to be metabolized before reaching the site of action
The aspect of counter-ions in peptides was not summarized in a such comprehensive review
Summary
Peptides along with proteins constitute the largest group of mediators of cellular processes making them pivotal for the functioning of many organisms For this reason, peptides are considered as attractive patterns for the development of new drugs and therapeutic routes [1,2]. That the breakthrough of peptide synthesis dates back to the 1960s (when the solid-phase synthesis was developed by Merrifield), peptides are still considered as poor drug candidates, mostly because of their poor bioavailability and the tendency to be metabolized before reaching the site of action Their synthesis is expensive and time-consuming, they are chemically unstable (pH and thermal degradation, oxidation), and difficult to maintain. Some approaches allow to modulate the pharmacokinetics and enhance their specificity [4] For this reason, more and more synthetic peptides and peptide-based drugs are reaching the market. This article discusses the role of counter-ions in peptides including drug formulation, the influence on physico-chemical properties and methods of counter-ion exchange, identification, and quantification
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