Florey Neuroscience Institutes, University of Melbourne, Melbourne, VIC 3010, Australia.
Amino Acids. 2012 Sep;43(3):1131-40. doi: 10.1007/s00726-012-1375-y. Epub 2012 Aug 2.
One of the most recognised and studied family of peptide hormones is the insulin superfamily. Within this family is the relaxin subfamily which comprises seven members: relaxin-1, -2 and -3 and insulin-like peptides 3, 4, 5 and 6. Besides exhibiting sequence similarities, each member exists as an active A-B heterodimer linked by three disulfide bonds. This mini-review is divided into three broad themes: an overview of all insulin superfamily members (including structural similarities); roles of each superfamily member and finally, a focus on the pleiotropic peptide hormone, human relaxin-2. In addition to promoting vasodilatory effects leading to evaluation in Phase III clinical trials for the treatment of acute heart failure, relaxin has recently been shown to be highly expressed by cancer cells, aiding in their proliferation, invasiveness and metastasis. These contrary effects of relaxin are discussed together with current efforts in the development of relaxin antagonists that may possess future therapeutic potential for the treatment of certain cancers.
胰岛素超家族是最被广泛认可和研究的肽类激素家族之一。在这个家族中，松弛素亚家族由七个成员组成：松弛素-1、-2 和 -3 以及胰岛素样肽 3、4、5 和 6。除了表现出序列相似性外，每个成员都以通过三个二硫键连接的活性 A-B 异二聚体形式存在。这篇迷你综述分为三个广泛的主题：胰岛素超家族所有成员的概述（包括结构相似性）；每个超家族成员的作用，最后，重点介绍多功能肽激素，人松弛素-2。除了促进血管舒张作用，导致在治疗急性心力衰竭的 III 期临床试验中进行评估外，松弛素最近还被显示在癌细胞中高度表达，有助于其增殖、侵袭和转移。本文将讨论松弛素的这些相反作用，并介绍松弛素拮抗剂的开发现状，这些拮抗剂可能具有治疗某些癌症的未来治疗潜力。
