Department of Neurosurgery, Otsu Municipal Hospital, Shiga, Japan.
Cell Mol Life Sci. 2011 Jan;68(2):195-203. doi: 10.1007/s00018-010-0518-0. Epub 2010 Sep 17.
Endothelin-1 is the most potent vasoconstrictor agent currently identified, and it was originally isolated and characterized from the culture media of aortic endothelial cells. Two other isoforms, termed endothelin-2 and endothelin-3, were subsequently identified, along with structural homologues isolated from the venom of Actractapis engaddensis known as the sarafotoxins. In this review, we will discuss the basic science of endothelins, endothelin-converting enzymes, and endothelin receptors. Only concise background information pertinent to clinical physician is provided. Next we will describe the pathophysiological roles of endothelin-1 in pulmonary arterial hypertension, heart failure, systemic hypertension, and female malignancies, with emphasis on ovarian cancer. The potential intervention with pharmacological therapeutics will be succinctly summarized to highlight the exciting pre-clinical and clinical studies within the endothelin field. Of note is the rapid development of selective endothelin receptor antagonists, which has led to an explosion of research in the field.
内皮素-1 是目前发现的最强血管收缩剂，最初从主动脉内皮细胞的培养基中分离并鉴定出来。随后又发现了另外两种同工型，称为内皮素-2 和内皮素-3，以及从 Actractapis engaddensis 的毒液中分离出来的结构类似物，称为沙罗毒素。在这篇综述中，我们将讨论内皮素、内皮素转换酶和内皮素受体的基础科学。仅提供与临床医生相关的简明背景信息。接下来，我们将描述内皮素-1 在肺动脉高压、心力衰竭、系统性高血压和女性恶性肿瘤（重点是卵巢癌）中的病理生理学作用。简要总结潜在的药物干预措施，以突出内皮素领域内令人兴奋的临床前和临床研究。值得注意的是，选择性内皮素受体拮抗剂的快速发展，使得该领域的研究呈爆炸式增长。
