文章基本信息

标题：Correlation of the biological activity and solution conformation of [Asp1,Ile5]- and [Phe4,Tyr8]angiotensin II
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作者：H E Bleich ; R J Freer ; S S Stafford 等
期刊名称：Proceedings of the National Academy of Sciences
印刷版ISSN：0027-8424
电子版ISSN：1091-6490
出版年度：1978
卷号：75
期号：8
页码：3630-3634
DOI：10.1073/pnas.75.8.3630
语种：English
出版社：The National Academy of Sciences of the United States of America
摘要：Angiotensin II is known to undergo a reversible conformational transition and a change in potency in rat uterus in vitro with pK approximately 6.5. We have shown by carbon-13 NMR that the conformational transition involves all-trans to partly cis isomerization of the His6-Pro7 peptide bond. Isomerization from all-trans at pH 6.8 to approximately 16% cis at pH 8.0 is therefore correlated with a 10-fold increase in biological activity for [Asp1,Ile5]-angiotensin II in rat uterus in vitro. Isomerization from all-trans at pH 6.8 to approximately 16% cis at pH 8.0 in the competitive inhibitor [Phe4,Tyr8]angiotensin II is correlated with exhibition of virtually no agonist activity at low pH to full agonist activity at high pH. An angiotensin II conformation with Pro7 in the cis form may therefore be the conformation with maximal binding or biological activity at the cellular receptor.