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Recent advances in the synthesis of C-terminally modified peptides.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-09-02 , DOI: 10.1039/d0ob01417f Christine A Arbour 1 , Lawrence G Mendoza 1 , Jennifer L Stockdill 1
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-09-02 , DOI: 10.1039/d0ob01417f Christine A Arbour 1 , Lawrence G Mendoza 1 , Jennifer L Stockdill 1
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C-Terminally modified peptides are important for the development and delivery of peptide-based pharmaceuticals because they impact peptide activity, stability, hydrophobicity, and membrane permeability. Additionally, the vulnerability of C-terminal esters to cleavage by endogenous esterases makes them excellent pro-drugs. Methods for post-SPPS C-terminal functionalization potentially enable access to libraries of modified peptides, facilitating tailoring of their solubility, potency, toxicity, and uptake pathway. Apparently minor structural changes can significantly impact the binding, folding, and pharmacokinetics of the peptide. This review summarizes developments in chemical methods for C-terminal modification of peptides published since the last review on this topic in 2003.
中文翻译：
C端修饰肽合成的最新进展。
C 末端修饰的肽对于肽类药物的开发和递送非常重要，因为它们会影响肽的活性、稳定性、疏水性和膜渗透性。此外，C 端酯易被内源酯酶裂解，这使得它们成为优异的前药。 SPPS C 端功能化后的方法可能能够获得修饰肽库，从而有助于调整其溶解度、效力、毒性和摄取途径。显然，微小的结构变化可以显着影响肽的结合、折叠和药代动力学。本综述总结了自 2003 年上一次关于该主题的综述以来发表的肽 C 末端修饰化学方法的进展。
更新日期：2020-09-30
中文翻译：
C端修饰肽合成的最新进展。
C 末端修饰的肽对于肽类药物的开发和递送非常重要，因为它们会影响肽的活性、稳定性、疏水性和膜渗透性。此外，C 端酯易被内源酯酶裂解，这使得它们成为优异的前药。 SPPS C 端功能化后的方法可能能够获得修饰肽库，从而有助于调整其溶解度、效力、毒性和摄取途径。显然，微小的结构变化可以显着影响肽的结合、折叠和药代动力学。本综述总结了自 2003 年上一次关于该主题的综述以来发表的肽 C 末端修饰化学方法的进展。
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