期刊论文详细信息
FEBS Letters | |
A novel ETA antagonist (BQ‐123) inhibits endothelin‐1‐induced phosphoinositide breakdown and DNA synthesis in rat vascular smooth muscle cells | |
Yano, Mitsuo1  Eguchi, Satoru2  Hirata, Yukio2  Marumo, Fumiaki2  Ihara, Masaki1  | |
[1] Central Research Laboratories, Banyu Pharmaceutical Co., 2-9-3 Shimomeguro, Meguroku, Tokyo 153, Japan;Second Department of Internal Medicine, Tokyo Medical and Dental University, 1-5-45 Yushima, Bunkyoku, Tokyo 113, Japan | |
关键词: Endothelin-1; Receptor antagonist; Inositol trisphosphate; DNA synthesis; Vascular smooth muscle cell; | |
DOI : 10.1016/0014-5793(92)80451-L | |
学科分类:生物化学/生物物理 | |
来源: John Wiley & Sons Ltd. | |
【 摘 要 】
The effects of a novel cyclic pentapeptide (BQ-123), an endothelin (ET) antagonist selective for the ETA 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 [125I]ET-1 to VSMC with the apparent K i of 4 × 10−9 M. BQ-123 dose-dependently inhibited formation of inositol-1,4,5-trisphosphate and [3H]thymidine uptake stimulated by ET-1. These data suggest that the ET-1-induced DNA synthesis in VSMC is mainly mediated by ETA receptor subtype.
【 授权许可】
Unknown
【 预 览 】
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