STRUCTURE-ACTIVITY-RELATIONSHIPS IN A SERIES OF MONOCYCLIC ENDOTHELIN ANALOGS

被引：8

作者：

CODY, WL

HE, JX

DEPUE, PL

RAPUNDALO, ST

HINGORANI, GP

DUDLEY, DT

HILL, KE

REYNOLDS, EE

DOHERTY, AM

机构：

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

[2] WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES,DEPT SIGNAL TRANSDUCT,ANN ARBOR,MI 48105

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)80156-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Monocyclic fragment analogues of endothelin-1 (ET-1) were prepared to explore the importance of the bicyclic structure of ET-1 to its binding affinity and functional activity. Most of the monocyclic analogues prepared showed low micro to high nanomolar binding affinities and were functional antagonists of ET-1 induced accumulation of inositol phosphates. However, one analogue possessed mixed antagonist/agonist activity at the two endothelin receptor subtypes.

引用

页码：567 / 572

页数：6

共 23 条

[1] CLONING AND EXPRESSION OF A CDNA-ENCODING AN ENDOTHELIN RECEPTOR [J].

ARAI, H ;

HORI, S ;

ARAMORI, I ;

OHKUBO, H ;

NAKANISHI, S .

NATURE, 1990, 348 (6303) :730-732

[2] DESIGN OF A FUNCTIONAL HEXAPEPTIDE ANTAGONIST OF ENDOTHELIN [J].

CODY, WL ;

DOHERTY, AM ;

HE, JX ;

DEPUE, PL ;

RAPUNDALO, ST ;

HINGORANI, GA ;

MAJOR, TC ;

PANEK, RL ;

DUDLEY, DT ;

HALEEN, SJ ;

LADOUCEUR, D ;

HILL, KE ;

FLYNN, MA ;

REYNOLDS, EE .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (17) :3301-3303

[3] MONOCYCLIC ENDOTHELINS - EXAMINATION OF THE IMPORTANCE OF THE INDIVIDUAL DISULFIDE RINGS [J].

CODY, WL ;

DOHERTY, AM ;

HE, XQ ;

RAPUNDALO, ST ;

HINGORANI, GP ;

PANEK, RL ;

MAJOR, TC .

JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1991, 17 :S62-S64

[4]

CODY WL, 1993, MED CHEM RES, V3, P154

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

DOHERTY, AM ;

CODY, WL ;

HE, JX ;

DEPUE, PL ;

LEONARD, DM ;

DUNBAR, JB ;

HILL, KE ;

FLYNN, MA ;

REYNOLDS, EE .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (04) :497-502

[6] ENDOTHELIN - A NEW CHALLENGE [J].

DOHERTY, AM .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (09) :1493-1508

[7] STRUCTURE ACTIVITY STUDIES OF THE C-TERMINAL REGION OF THE ENDOTHELINS AND THE SARAFOTOXINS [J].

DOHERTY, AM ;

CODY, WL ;

LEITZ, NL ;

DEPUE, PL ;

TAYLOR, MD ;

RAPUNDALO, ST ;

HINGORANI, GP ;

MAJOR, TC ;

PANEK, RL ;

TAYLOR, DG .

JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1991, 17 :S59-S61

[8] STRUCTURE-ACTIVITY-RELATIONSHIPS OF C-TERMINAL ENDOTHELIN HEXAPEPTIDE ANTAGONISTS [J].

DOHERTY, AM ;

CODY, WL ;

DEPUE, PL ;

HE, JX ;

WAITE, LA ;

LEONARD, DM ;

LEITZ, NL ;

DUDLEY, DT ;

RAPUNDALO, ST ;

HINGORANI, GP ;

HALEEN, SJ ;

LADOUCEUR, DM ;

HILL, KE ;

FLYNN, MA ;

REYNOLDS, EE .

JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (18) :2585-2594

[9]

FOK KF, 1990, PEPTIDES CHEM STRUCT, P269

[10] CHARACTERIZATION OF A CORONARY VASOCONSTRICTOR PRODUCED BY CULTURED ENDOTHELIAL-CELLS [J].

HICKEY, KA ;

RUBANYI, G ;

PAUL, RJ ;

HIGHSMITH, RF .

AMERICAN JOURNAL OF PHYSIOLOGY, 1985, 248 (05) :C550-C556

← 1 2 3 →