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Enzymatic pathways involved in the generation of endothelin-1(1-31) from exogenous big endothelin-1 in the rabbit aorta.家兔主动脉中参与从外源性大内皮素-1生成内皮素-1(1-31)的酶促途径。
Br J Pharmacol. 2006 Jun;148(4):527-35. doi: 10.1038/sj.bjp.0706735. Epub 2006 Apr 24.
2
Differential role of TGF-beta1/bFGF and ET-1 in graft fibrosis in heart failure patients.转化生长因子-β1/碱性成纤维细胞生长因子和内皮素-1在心力衰竭患者移植纤维化中的差异作用
Am J Transplant. 2005 Sep;5(9):2185-92. doi: 10.1111/j.1600-6143.2005.01006.x.
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Native and oxidized low-density lipoproteins stimulate endothelin-converting enzyme-1 expression in human endothelial cells.天然和氧化型低密度脂蛋白刺激人内皮细胞中内皮素转换酶-1的表达。
Biochem Biophys Res Commun. 2005 Sep 2;334(3):747-53. doi: 10.1016/j.bbrc.2005.06.163.
4
Endothelin antagonism in pulmonary hypertension, heart failure, and beyond.内皮素拮抗作用在肺动脉高压、心力衰竭及其他病症中的应用
Heart. 2005 Jun;91(6):825-31. doi: 10.1136/hrt.2004.053991.
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Crosstalk between mesangial and endothelial cells: angiotensin II down-regulates endothelin-converting enzyme 1.系膜细胞与内皮细胞之间的相互作用：血管紧张素II下调内皮素转换酶1。
Cell Physiol Biochem. 2005;15(1-4):135-44. doi: 10.1159/000083646.
6
Sustained improvement of cardiac function and prevention of cardiac remodeling after long-term dual ECE-NEP inhibition in rats with congestive heart failure.在充血性心力衰竭大鼠中，长期双重内皮素转换酶-中性肽链内切酶抑制后心脏功能的持续改善及心脏重塑的预防。
J Cardiovasc Pharmacol. 2004 Apr;43(4):489-94. doi: 10.1097/00005344-200404000-00003.
7
Increased expression of endothelin-converting enzyme-1c isoform in response to high glucose levels in endothelial cells.内皮细胞中内皮素转换酶-1c亚型在高糖水平刺激下表达增加。
J Vasc Res. 2004 Mar-Apr;41(2):131-40. doi: 10.1159/000077132. Epub 2004 Feb 27.
8
The effects of phosphoramidon on the expression of human endothelin-converting enzyme-1 (ECE-1) isoforms.磷酰胺素对人内皮素转换酶-1（ECE-1）同工型表达的影响。
J Cardiovasc Pharmacol. 2003 Jul;42(1):136-41. doi: 10.1097/00005344-200307000-00021.
9
Shear stress attenuates endothelin and endothelin-converting enzyme expression through oxidative stress.剪切应力通过氧化应激减弱内皮素和内皮素转换酶的表达。
Regul Pept. 2003 Mar 28;111(1-3):13-9. doi: 10.1016/s0167-0115(02)00219-7.
10
Hydrogen peroxide regulation of bovine endothelin-converting enzyme-1.过氧化氢对牛内皮素转化酶-1的调节作用
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肽酶抑制剂CGS-26303通过大内皮素-1的积累增加内皮细胞中内皮素转换酶-1的表达。

The peptidase inhibitor CGS-26303 increases endothelin converting enzyme-1 expression in endothelial cells through accumulation of big endothelin-1.

作者信息

Raoch V, Martinez-Miguel P, Arribas-Gomez I, Rodriguez-Puyol M, Rodriguez-Puyol D, Lopez-Ongil S

机构信息

Hospital Universitario Principe de Asturias, Research Unit and Nephrology section, Ctra. Alcala-Meco s/n, Madrid, Spain.

出版信息

Br J Pharmacol. 2007 Oct;152(3):313-22. doi: 10.1038/sj.bjp.0707398. Epub 2007 Jul 23.

DOI:10.1038/sj.bjp.0707398
PMID:17643133
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2042959/
Abstract

BACKGROUND AND PURPOSE

CGS-26303 inhibits endothelin converting enzyme (ECE)-1 more specifically than phosphoramidon. We have studied the effect of CGS-26303 on ECE-1 expression in bovine aortic endothelial cells.

METHODS

ECE-1 activity and big endothelin (ET)-1 levels were measured by ELISA, ECE-1 expression using western and northern blot and promoter activity using transfection assays.

KEY RESULTS

ECE-1 activity was completely inhibited by CGS-26303 25 microM and phosphoramidon 100 microM. CGS-26303 and phosphoramidon, though not thiorphan, a neutral endopeptidase (NEP) inhibitor, stimulated ECE-1 expression in cells (maximal effect at 16 h, 25 microM). Cycloheximide abolished that effect. CGS-26303 induced ECE-1 mRNA expression and ECE-1 promoter activity. CGS-35066, a selective ECE-1 inhibitor, mimicked the effects of CGS-26303, suggesting that the effect was specific to ECE-1 inhibition. Big ET-1 accumulated in the cells and in the supernatants after CGS-26303 treatment. Neither exogenously added ET-1 nor the blockade of their receptors with bosentan modified ECE-1 protein. When big ET-1 was added to cells, significant increases in ECE-1 protein content and ECE-1 promoter activity were found. Bosentan did not block those effects. CGS-26303 did not modify prepro-ET-1 expression. CGS-26303 and big ET-1 induced the same effects in human endothelial cells, at lower doses.

CONCLUSIONS

These results suggest that the accumulation of big ET-1 is responsible for the effects of CGS-26303 on ECE-1 and they did not depend on NEP blockade. Changes in ECE-1 protein after the administration of CGS-26303 could lead to a decreased response in long-term treatments.

摘要

背景与目的

CGS - 26303比磷酰胺素更特异性地抑制内皮素转换酶（ECE）-1。我们研究了CGS - 26303对牛主动脉内皮细胞中ECE - 1表达的影响。

方法

通过酶联免疫吸附测定（ELISA）测量ECE - 1活性和大内皮素（ET）-1水平，利用蛋白质免疫印迹法和Northern印迹法检测ECE - 1表达，通过转染实验检测启动子活性。

主要结果

25微摩尔的CGS - 26303和100微摩尔的磷酰胺素可完全抑制ECE - 1活性。CGS - 26303和磷酰胺素，而非中性内肽酶（NEP）抑制剂硫磷酰胺，可刺激细胞中ECE - 1的表达（在16小时时，25微摩尔时达到最大效应）。放线菌酮可消除该效应。CGS - 26303诱导ECE - 1信使核糖核酸（mRNA）表达和ECE - 1启动子活性。选择性ECE - 1抑制剂CGS - 35066模拟了CGS - 26303的作用，表明该效应是ECE - 1抑制所特有的。CGS - 26303处理后，大ET - 1在细胞和上清液中积累。外源性添加的ET - 1或用波生坦阻断其受体均未改变ECE - 1蛋白。当向细胞中添加大ET - 1时，发现ECE - 1蛋白含量和ECE - 1启动子活性显著增加。波生坦未阻断这些效应。CGS - 26303未改变前内皮素原（prepro - ET）-1的表达。CGS - 26303和大ET - 1在较低剂量下对人内皮细胞诱导相同的效应。

结论

这些结果表明，大ET - 1的积累是CGS - 26303对ECE - 1产生作用的原因，且它们不依赖于NEP阻断。给予CGS - 26303后ECE - 1蛋白的变化可能导致长期治疗中反应降低。