کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370666 981824 2011 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Substitution of the GalNAc-α-O-Thr11 residue in drosocin with O-linked glyco-peptoid residue: Effect on antibacterial activity and conformational change
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Substitution of the GalNAc-α-O-Thr11 residue in drosocin with O-linked glyco-peptoid residue: Effect on antibacterial activity and conformational change
چکیده انگلیسی

One of the obvious disadvantages of natural peptides is their liability to proteases. Among the several solutions for this issue, peptoids or oligomers of N-substituted glycine have emerged as a promising tool that may enhance the stability of proteolysis-susceptible natural peptides. We have synthesized the drosocin and its glyco-peptoid analogues linked O-GalNAc at the Thr11 residue. One of our glyco-peptoid analogues showed an increased antibacterial activity by the modification of the Thr11 residue with glyco-peptoid. Structure–activity relationship studies revealed that the antibacterial activity by glyco-peptoid drosocin requires three key elements: free hydroxyl group on the carbohydrate moiety, γ-methyl group of the Thr11 residue derivative and (S)-configuration over (R)-configuration.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 20, 15 October 2011, Pages 6148–6153
نویسندگان
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