通过血清蛋白酶控制聚乙二醇化前药中治疗性肽的受控全身释放。
Controlled systemic release of therapeutic peptides from PEGylated prodrugs by serum proteases.
机构信息
Institut für Bioanalytische Chemie, Zentrum für Biotechnologie und Biomedizin, Universität Leipzig, Deutscher Platz 5, 04103 Leipzig, Germany.
出版信息
Angew Chem Int Ed Engl. 2013 Jul 15;52(29):7597-9. doi: 10.1002/anie.201301533. Epub 2013 Jun 13.
A novel concept to release peptidic drugs systemically by serum proteases from a PEGylated precursor makes it possible to tune release kinetics to fit the medical needs. Drug release depends on the size of the PEG polymer and the sequence and length of the peptide linker. The antimicrobial activities of the prodrugs were even better than those of the free peptides, whereas direct PEGylation abolished the peptide activity.
通过血清蛋白酶从聚乙二醇化前体系统释放肽类药物的新概念，使得调节释放动力学以适应医疗需求成为可能。药物释放取决于 PEG 聚合物的大小以及肽连接子的序列和长度。前药的抗菌活性甚至优于游离肽，而直接聚乙二醇化则使肽失去活性。
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