文章：

内皮素轴：在癌症中的新作用

The endothelin axis: emerging role in cancer

原文发布日期：2003-02-01

DOI: 10.1038/nrc990

类型: Review Article

开放获取: 否

要点：

1. Studies have demonstrated the role of the ET axis in a wide variety of diseases, including cancer.
2. ET_A-receptor activation by ET-1 contributes to tumour growth and progression, inducing cell proliferation, survival, angiogenesis and metastatic spread, indicating that ET_A-receptor blockade might improve cancer treatment.
3. In Phase I and II clinical studies, ET_A-receptor antagonists can be administered orally, once a day, and have a favourable tolerability profile.
4. Preliminary data from clinical trials are promising.
5. Studies are underway to better define the role and ET-receptor antagonists in the treatment of malignant diseases.

要点翻译：

1. 研究表明，内皮素轴在多种疾病（包括癌症）中发挥作用。
2. 内皮素-1激活ETA受体可促进肿瘤生长和进展，诱导细胞增殖、存活、血管生成和转移扩散，表明阻断ETA受体或可改善癌症治疗。
3. 在I期和II期临床研究中，ETA受体拮抗剂可每日一次口服给药，且耐受性良好。
4. 临床试验的初步数据令人鼓舞。
5. 目前正在进行研究，以更明确地界定内皮素受体拮抗剂在恶性疾病治疗中的作用。

英文摘要：

Collectively, the endothelins and their receptors — referred to as the endothelin (ET) axis — have key physiological functions in normal tissue, acting as modulators of vasomotor tone, tissue differentiation, development, cell proliferation and hormone production. Based on new data, the ET axis also functions in the growth and progression of various tumours. Preliminary results from clinical trials, such as those with atrasentan — an ETA-receptor antagonist — in prostate cancer, are encouraging. The place of ET-receptor antagonists in cancer therapy for a range of malignancies merits further investigation.

摘要翻译： 

内皮素及其受体统称为内皮素（ET）轴，在正常组织中具有关键的生理功能，可作为血管张力、组织分化、发育、细胞增殖和激素产生的调节因子。最新数据表明，ET轴也参与多种肿瘤的生长和进展。临床试验的初步结果令人鼓舞，例如在前列腺癌中使用ETA受体拮抗剂atrasentan的研究。ET受体拮抗剂在多种恶性肿瘤治疗中的地位值得进一步研究。

原文链接：

The endothelin axis: emerging role in cancer