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Design and synthesis of an amide-linked angiotensin II analogue with 3,5 side chain bridge:structural resemblance of ring cluster conformation with AT_1 non-peptide antagonists

机译:与3,5侧链桥的酰胺连接血管紧张素II类似物的设计与合成:与AT_1非肽拮抗剂的环形簇构象的结构相似

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摘要

The novel amide linked Angiotensin II cyclic analogue c-(3,5)-[Sar~1-Lys~3-Glu~5-Ile~8]-ANG II (Figure 1) has been designed,synthesized and bioassayed in anesthetized rabbits.The aim of this work was to investigate furthermore the role of a ring cluster receptor conforation in agonist activity and shed light to intriguing differences in activity and conformation upon replacement of aromatic residue Phe with aliphatic Ile.
机译:新型酰胺连接血管紧张素II环状类似物C-(3,5) - [SAR〜1-LYS〜3-GLU〜5-ILE〜8] - ang II(图1)在麻醉的兔子中合成和生物测量。该工作的目的是进一步研究戒指聚类受体对激动剂活性和脱光的作用,并在用脂族ILe替代芳族残基PHE时对活性和构象的敏化差异。

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