STRUCTURE-ACTIVITY-RELATIONSHIPS OF MONOCYCLIC ENDOTHELIN ANALOGS

被引：41

作者：

HUNT, JT ^{[1
]}

LEE, VG ^{[1
]}

STEIN, PD ^{[1
]}

HEDBERG, A ^{[1
]}

LIU, ECK ^{[1
]}

MCMULLEN, D ^{[1
]}

MORELAND, S ^{[1
]}

机构：

[1] BRISTOL MYERS SQUIBB,PHARMACEUT RES INST,DEPT PHARMACOL,PRINCETON,NJ 08543

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)81085-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Analogs of monocyclic ET-1 (Ala3,11, Nle7) containing alanine substitutions were prepared and assayed for vasoconstrictor and receptor binding activity. Analogs substituted at residues Glu10, Phe14, Leu17 and Aspl8 showed significant affinity for the receptor at concentrations below those at which agonism was observed. To the extent that structure-activity relationships of monocyclic and bicyclic ETs can be compared, this study suggests that residues 10, 14, 17 and 18 are candidate sites for exploration of peptides which show ET receptor antagonism.

引用

页码：33 / 38

页数：6

共 11 条

[1] MODIFICATIONS OF POSITION-12 IN PARATHYROID-HORMONE AND PARATHYROID-HORMONE RELATED PROTEIN - TOWARD THE DESIGN OF HIGHLY POTENT ANTAGONISTS
CHOREV, M
GOLDMAN, ME
MCKEE, RL
ROUBINI, E
LEVY, JJ
GAY, CT
REAGAN, JE
FISHER, JE
CAPORALE, LH
GOLUB, EE
CAULFIELD, MP
NUTT, RF
ROSENBLATT, M
[J]. BIOCHEMISTRY, 1990, 29 (06) : 1580 - 1586
[2] FIRTH JD, 1988, LANCET, V2, P1179
[3] RECEPTOR-BINDING ACTIVITY AND CYTOSOLIC FREE CALCIUM RESPONSE BY SYNTHETIC ENDOTHELIN ANALOGS IN CULTURED RAT VASCULAR SMOOTH-MUSCLE CELLS
HIRATA, Y
YOSHIMI, H
EMORI, T
SHICHIRI, M
MARUMO, F
WATANABE, TX
KUMAGAYE, S
NAKAJIMA, K
KIMURA, T
SAKAKIBARA, S
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 160 (01) : 228 - 234
[4] STRUCTURE-ACTIVITY-RELATIONSHIPS OF ENDOTHELIN - IMPORTANCE OF THE C-TERMINAL MOIETY
KIMURA, S
KASUYA, Y
SAWAMURA, T
SHINMI, O
SUGITA, Y
YANAGISAWA, M
GOTO, K
MASAKI, T
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1988, 156 (03) : 1182 - 1186
[5] GLOMERULAR ACTIONS OF ENDOTHELIN INVIVO
KON, V
YOSHIOKA, T
FOGO, A
ICHIKAWA, I
[J]. JOURNAL OF CLINICAL INVESTIGATION, 1989, 83 (05) : 1762 - 1767
[6] KUMAGAYE SI, 1988, INT J PEPT PROT RES, V32, P519
[7] STRUCTURE-ACTIVITY RELATIONSHIP OF ENDOTHELIN - IMPORTANCE OF CHARGED GROUPS
NAKAJIMA, K
KUBO, S
KUMAGAYE, S
NISHIO, H
TSUNEMI, M
INUI, T
KURODA, H
CHINO, N
WATANABE, TX
KIMURA, T
SAKAKIBARA, S
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 163 (01) : 424 - 429
[8] CHARACTERIZATION OF CONTRACTILE RESPONSES TO ENDOTHELIN IN HUMAN CEREBRAL-ARTERIES - IMPLICATIONS FOR CEREBRAL VASOSPASM
PAPADOPOULOS, SM
GILBERT, LL
WEBB, RC
DAMATO, CJ
[J]. NEUROSURGERY, 1990, 26 (05) : 810 - 815
[9] PLASMA ENDOTHELIN LEVELS IN HYPERTENSION AND CHRONIC-RENAL-FAILURE
SHICHIRI, M
HIRATA, Y
ANDO, K
EMORI, T
OHTA, K
KIMOTO, S
OGURA, M
INOUE, A
MARUMO, F
[J]. HYPERTENSION, 1990, 15 (05) : 493 - 496
[10] EFFECTS OF CALCIUM ENTRY BLOCKERS ON CONTRACTIONS EVOKED BY ENDOTHELIN-1, [ALA3,11]ENDOTHELIN-1 AND [ALA1,15]ENDOTHELIN-1 IN RAT ISOLATED AORTA
TOPOUZIS, S
PELTON, JT
MILLER, RC
[J]. BRITISH JOURNAL OF PHARMACOLOGY, 1989, 98 (02) : 669 - 677

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