Synthesis of Biologically Active Peptide Nucleic Acid-Peptide Conjugates by Sortase-Mediated Ligation

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• 作者：Stephan Pritz ; Yvonne Wolf ; Oliver Kraetke ; Jana Klose ; Michael Bienert ; Michael Beyermann
• 刊名：Journal of Organic Chemistry
• 出版年：2007
• 出版时间：May 11, 2007
• 年：2007
• 卷：72
• 期：10
• 页码：3909 - 3912
• 全文大小：108K
• 年卷期：v.72,no.10(May 11, 2007)
• ISSN：1520-6904

文摘

Sortase A is a transpeptidase that cleaves at a pentapeptide-motif and subsequently transfers the acyl component to anucleophile containing N-terminal oligoglycines. We investigate the reaction conditions of the sortase-mediated ligationand demonstrate a useful application by the synthesis of apeptide nucleic acid-cell-penetrating peptide chimera, thereaction equilibrium of which can be shifted in favor of theproduct by dialyzing out the low molecular weight byproduct.The synthesized conjugate exhibits dose-dependent antisenseactivity.