Synthesis of Biologically Active Peptide Nucleic Acid−Peptide Conjugates by Sortase-Mediated Ligation
2007; American Chemical Society; Volume: 72; Issue: 10 Linguagem: Inglês
10.1021/jo062331l
ISSN1520-6904
AutoresS. Pritz, Yvonne Wolf, Oliver Kraetke, Jana Klose, Michael Bienert, Michael Beyermann,
Tópico(s)Machine Learning in Bioinformatics
ResumoSortase A is a transpeptidase that cleaves at a pentapeptide-motif and subsequently transfers the acyl component to a nucleophile containing N-terminal oligoglycines. We investigate the reaction conditions of the sortase-mediated ligation and demonstrate a useful application by the synthesis of a peptide nucleic acid−cell-penetrating peptide chimera, the reaction equilibrium of which can be shifted in favor of the product by dialyzing out the low molecular weight byproduct. The synthesized conjugate exhibits dose-dependent antisense activity.
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