DESIGN OF C-TERMINAL PEPTIDE ANTAGONISTS OF ENDOTHELIN - STRUCTURE-ACTIVITY-RELATIONSHIPS OF ET-1[16-21,D-HIS16]

被引：24

作者：

DOHERTY, AM ^{[1
]}

CODY, WL ^{[1
]}

HE, JX ^{[1
]}

DEPUE, PL ^{[1
]}

LEONARD, DM ^{[1
]}

DUNBAR, JB ^{[1
]}

HILL, KE ^{[1
]}

FLYNN, MA ^{[1
]}

REYNOLDS, EE ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)81215-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have previously described structure-activity relationships in the hydrophobic C-terminal hexapeptide region of ET-1 known to be highly important for receptor recognition. A mono-D-amino acid scan of ET[16-21] revealed that a D-His16 substitution gave rise to endothelin antagonists. We will describe the discovery and development of further antagonists in this series.

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页码：497 / 502

页数：6

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