IMPORTANCE OF SECONDARY STRUCTURE FOR ENDOTHELIN BINDING AND FUNCTIONAL-ACTIVITY

被引：14

作者：

PANEK, RL ^{[1
]}

MAJOR, TC ^{[1
]}

TAYLOR, DG ^{[1
]}

HINGORANI, GP ^{[1
]}

DUNBAR, JB ^{[1
]}

DOHERTY, AM ^{[1
]}

RAPUNDALO, ST ^{[1
]}

机构：

[1] WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT CHEM,ANN ARBOR,MI 48105

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1992年 / 183卷 / 02期

关键词：

D O I：

10.1016/0006-291X(92)90520-U

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

ET-1[16-Phe] and ET-1[12-Pro] were prepared in order to investigate the importance of secondary structure of ET-1 for receptor binding and function. ET-1[16-Phe] displayed the greatest binding and contractile potency of the ET-analogs tested in rabbit pulmonary artery, rat aorta, and rat left atria. ET-1[12-Pro] also exhibited low nanomolar binding in these tissues but showed less contractile activity than ET-1[16-Phe] or ET-1. The results indicate that the helical region between residues Lys9 and Cys15 of ET-1 is not critical for receptor binding and functional activity. However, replacement of His16 with Phe altered the charge characteristics of the C-terminal region of ET-1 producing the most potent ET-1 analog yet reported. © 1992.

引用

页码：572 / 576

页数：5

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