Analysis of the mechanism by nobel regulators of endothelin receptor signaling

内皮素受体信号传导的诺贝尔调节剂的机制分析

• 批准号: 09680613
• 负责人: KIMURA Sadao
• 金额: $ 2.11万
• 依托单位: Chiba University Graduate School of Medicine
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 1997
• 资助国家: 日本
• 起止时间: 1997 至 1998
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-09680613/
• 关键词: Endothelin; Endothelin receptors; Endothelin receptor antagonists; Desensitization; Binding experiment; Regulators of G protein signaling; G蛋白質共役受容体キナーゼ

(1) [^<25>I]endothelin(ET)-l binding and functional properties of CHO cells stably coexpressing ETA and ETB receptors were studied. The results provide a new insight into relationship between ET receptors and their ligands, demonstrating that ET-1 displaced from ETB receptors by ETB receptor antagonists is trapped by ETA receptors and causes ETA receptor-mediated responses. (2) RGS (regulator of G protein signaling) genes which present in heart and smooth muscle were transiently expressed into cells and their suppression activities of ET-1-mediated responses were evidenced.

(1)研究<25>了稳定共表达ETA和ETB受体的CHO细胞的[^ I]内皮素（ET）-1结合和功能特性。这些结果为ET受体与其配体之间的关系提供了新的见解，表明ETB受体拮抗剂从ETB受体上取代的ET-1被ETA受体捕获并引起ETA受体介导的反应。(2)存在于心脏和平滑肌中的RGS（regulator of G protein signaling）基因在细胞中瞬时表达，证实了其对ET-1介导的反应的抑制活性。

项目成果

Tanaka, H., Moroi, K., Nishiyama, M., Kimura, S.et al.: "Novel mutations of the endothelin B receptor gene in patients with Hirschsprung disease and their characterization." J.Biol.Chem.273. 11378-11383 (1998)

Tanaka, H.、Moroi, K.、Nishiyama, M.、Kimura, S.等人：“先天性巨结肠患者内皮素 B 受体基因的新突变及其特征。”

木村 定雄: "エンドセリン研究の最前線" Progress in Medicine. 18. 2073-2081 (1998)

木村贞夫：“内皮素研究的前沿”医学进展18。2073-2081（1998）。

Tanaka,H., Moroi,K., Nishiyama,M., Kimura,S.ら: "Novel mutations of the endothelin B receptor gene in patients with Hirschsprung disease and their characterization." J.Biol.Chem.印刷中. (1998)

Tanaka, H.、Moroi, K.、Nishiyama, M.、Kimura, S. 等人：“先天性巨结肠症患者的内皮素 B 受体基因的新突变及其特征，发表于《J. Biol》”。 （1998）

T.Shibasaki, K.Moroi, M.Nishiyama, J.Zhou, A.Sakamoto, T.Masaki, K.Itoh, T.Haga, S.Kimura.: "Characterization of the carboxyl terminal-truncated endothelin B receptor coexpressed with G protein-coupled receptor kinase 2." Biochem.Mol.Biol.Int.(in press).

T.Shibasaki、K.Moroi、M.Nishiyama、J.Zhou、A.Sakamoto、T.Masaki、K.Itoh、T.Haga、S.Kimura.：“与共表达的羧基末端截短的内皮素 B 受体的表征

Yamamoto,T., Nozaki-Taguchi,N. and Kimura,S.: "Analgesic effect of intrathecally administered nociceptin,an opioid receptor-likel receptor agonist,in the rat formalin test." Neuroscience. 81. 249-254 (1997)

山本，T.，野崎田口，N.