A NOVEL ETA ANTAGONIST (BQ-123) INHIBITS ENDOTHELIN-1-INDUCED PHOSPHOINOSITIDE BREAKDOWN AND DNA-SYNTHESIS IN RAT VASCULAR SMOOTH-MUSCLE CELLS

被引：95

作者：

EGUCHI, S

HIRATA, Y

IHARA, M

YANO, M

MARUMO, F

机构：

[1] TOKYO MED & DENT UNIV,DEPT INTERNAL MED 2,DIV ENDOCRINE HYPERTENS,1-5-45 YUSHIMA,BUNKYO KU,TOKYO 113,JAPAN

[2] BANYO PHARMACEUT CO,CENT RES LABS,MEGURO KU,TOKYO 153,JAPAN

来源：

FEBS LETTERS | 1992年 / 302卷 / 03期

关键词：

ENDOTHELIN-1; RECEPTOR ANTAGONIST; INOSITOL TRISPHOSPHATE; DNA SYNTHESIS; VASCULAR SMOOTH MUSCLE CELL;

D O I：

10.1016/0014-5793(92)80451-L

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：

The effects of a novel cyclic pentapeptide (BQ-123), an endothelin (ET) antagonist selective for the ET(A) receptor subtype, on phosphoinositide breakdown and DNA synthesis stimulated by ET-1 were studied in cultured rat vascular smooth muscle cells (VSMC). BQ-123 competitively inhibited the binding of [I-125]ET-1 to VSMC with the apparent K(i) of 4 x 10(-9) M. BQ-123 dose-dependently inhibited formation of inositol-1,4,5-trisphosphate and [H-3]thymidine uptake stimulated by ET-1. These data suggest that the ET-1-induced DNA synthesis in VSMC is mainly mediated by ET(A) receptor subtype.

引用

页码：243 / 246

页数：4

共 16 条

[1] CLONING AND EXPRESSION OF A CDNA-ENCODING AN ENDOTHELIN RECEPTOR
ARAI, H
HORI, S
ARAMORI, I
OHKUBO, H
NAKANISHI, S
[J]. NATURE, 1990, 348 (6303) : 730 - 732
[2] GROWTH-FACTOR ACTIVITY OF ENDOTHELIN ON VASCULAR SMOOTH-MUSCLE
BOBIK, A
GROOMS, A
MILLAR, JA
MITCHELL, A
GRINPUKEL, S
[J]. AMERICAN JOURNAL OF PHYSIOLOGY, 1990, 258 (03): : C408 - C415
[3] SPECIFIC RECEPTORS FOR ATRIAL NATRIURETIC FACTOR (ANF) IN CULTURED VASCULAR SMOOTH-MUSCLE CELLS OF RAT AORTA
HIRATA, Y
TOMITA, M
YOSHIMI, H
IKEDA, M
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1984, 125 (02) : 562 - 568
[4] INTERACTION OF ENDOTHELIN ISOPEPTIDES WITH VASCULAR ENDOTHELIN-1 RECEPTOR
HIRATA, Y
YOSHIMI, H
TAKAGI, Y
KANNO, K
EGUCHI, S
MARUMO, F
[J]. BIOMEDICAL RESEARCH-TOKYO, 1990, 11 (03): : 195 - 198
[5] ENDOTHELIN IS A POTENT MITOGEN FOR RAT VASCULAR SMOOTH-MUSCLE CELLS
HIRATA, Y
TAKAGI, Y
FUKUDA, Y
MARUMO, F
[J]. ATHEROSCLEROSIS, 1989, 78 (2-3) : 225 - 228
[6] CELLULAR MECHANISM OF ACTION BY A NOVEL VASOCONSTRICTOR ENDOTHELIN IN CULTURED RAT VASCULAR SMOOTH-MUSCLE CELLS
HIRATA, Y
YOSHIMI, H
TAKATA, S
WATANABE, TX
KUMAGAI, S
NAKAJIMA, K
SAKAKIBARA, S
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1988, 154 (03) : 868 - 875
[7] BIOLOGICAL PROFILES OF HIGHLY POTENT NOVEL ENDOTHELIN ANTAGONISTS SELECTIVE FOR THE ETA RECEPTOR
IHARA, M
NOGUCHI, K
SAEKI, T
FUKURODA, T
TSUCHIDA, S
KIMURA, S
FUKAMI, T
ISHIKAWA, K
NISHIKIBE, M
YANO, M
[J]. LIFE SCIENCES, 1992, 50 (04) : 247 - 255
[8] AN ENDOTHELIN RECEPTOR (ETA) ANTAGONIST ISOLATED FROM STREPTOMYCES-MISAKIENSIS
IHARA, M
FUKURODA, T
SAEKI, T
NISHIKIBE, M
KOJIRI, K
SUDA, H
YANO, M
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 178 (01) : 132 - 137
[9] THE HUMAN ENDOTHELIN FAMILY - 3 STRUCTURALLY AND PHARMACOLOGICALLY DISTINCT ISOPEPTIDES PREDICTED BY 3 SEPARATE GENES
INOUE, A
YANAGISAWA, M
KIMURA, S
KASUYA, Y
MIYAUCHI, T
GOTO, K
MASAKI, T
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (08) : 2863 - 2867
[10] ENDOTHELIN-1 AND VASCULITIS
KANNO, K
HIRATA, Y
NUMANO, F
EMORI, T
OHTA, K
SHICHIRI, M
MARUMO, F
[J]. JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, 1990, 264 (22): : 2868 - 2868

← 1 2 →