کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365289 | 981557 | 2006 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Short pseudopeptides containing turn scaffolds with high AT2 receptor affinity
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Two pentapeptides, Ac-Tyr-Ile-His-Pro-Phe/Ile, were synthesized and shown to have angiotensin II AT2 receptor affinity and agonistic activity. Based on these peptides, a new series of 13 pseudopeptides was synthesized via introduction of five different turn scaffolds replacing the Tyr-Ile amino acid residues. Pharmacological evaluation disclosed subnanomolar affinities for some of these compounds at the AT2 receptor. Substitution of Phe by Ile in this series of ligands enhanced the AT2 receptor affinity of all compounds. These results suggest that the C-terminal amino acid residues can be elaborated on to enhance the AT2 receptor affinity in truncated Ang II analogues.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 17, 1 September 2006, Pages 5963–5972
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 17, 1 September 2006, Pages 5963–5972
نویسندگان
Jennie Georgsson, Ulrika Rosenström, Charlotta Wallinder, Hélène Beaudry, Bianca Plouffe, Gunnar Lindeberg, Milad Botros, Fred Nyberg, Anders Karlén, Nicole Gallo-Payet, Anders Hallberg,