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松弛素:一种古老蛋白的新病理生理学方面和药理学前景。

Relaxin: new pathophysiological aspects and pharmacological perspectives for an old protein.

机构信息

Department of Internal Medicine, University of Messina, Via Consolare Valeria, 1, 98100, Italy.

出版信息

Med Res Rev. 2014 Jan;34(1):77-105. doi: 10.1002/med.21277. Epub 2013 Feb 11.

Abstract

Human relaxin-2 (hereafter simply defined as "relaxin") is a 6-kDa peptidic hormone best known for the physiological role played during pregnancy in the growth and differentiation of the reproductive tract and in the renal and systemic hemodynamic changes. This factor can also be involved in the pathophysiology of arterial hypertension and heart failure, in the molecular pathways of fibrosis and cancer, and in angiogenesis and bone remodeling. It belongs to the relaxin peptide family, whose members comprehensively exert numerous effects through interaction with different types of receptors, classified as relaxin family peptide (RXFP) receptors (RXFP1, RXFP2, RXFP3, RXFP4). Research looks toward the in-depth examination and complete understanding of relaxin in its various pleiotropic actions. The intent is to evaluate the likelihood of employing this substance for therapeutic purposes, for instance in diseases where a deficit could be part of the underlying pathophysiological mechanisms, also avoiding any adverse effect. Relaxin is already being considered as a promising drug, especially in acute heart failure. A careful study of the different RXFPs and their receptors and the comprehension of all biological activities of these hormones will probably provide new drugs with a potential wide range of therapeutic applications in the near future.

摘要

人松弛素-2(以下简称“松弛素”)是一种 6kDa 的肽类激素,在妊娠期间在生殖道的生长和分化以及肾脏和全身血液动力学变化中发挥生理作用而广为人知。该因子还可能参与动脉高血压和心力衰竭的病理生理学、纤维化和癌症的分子途径以及血管生成和骨重塑。它属于松弛素肽家族,其成员通过与不同类型的受体相互作用全面发挥多种作用,这些受体被分类为松弛素家族肽(RXFP)受体(RXFP1、RXFP2、RXFP3、RXFP4)。研究着眼于深入检查和全面了解松弛素在其各种多功能作用中的作用。目的是评估该物质用于治疗目的的可能性,例如在潜在病理生理机制中可能存在缺陷的疾病中,同时避免任何不良反应。松弛素已被认为是一种很有前途的药物,尤其是在急性心力衰竭中。仔细研究不同的 RXFPs 及其受体,并理解这些激素的所有生物学活性,可能会在不久的将来提供具有广泛治疗应用潜力的新药。

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