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激活素受体信号通路及其抑制的原则。

Principles of the activin receptor signaling pathway and its inhibition.

机构信息

Department of Biomedicine, Aarhus University, Department of Respiratory Diseases and Allergy, Aarhus University Hospital, Wilhelm Meyers Allé, DK-8000, Aarhus, Denmark.

出版信息

Cytokine Growth Factor Rev. 2021 Aug;60:1-17. doi: 10.1016/j.cytogfr.2021.04.001. Epub 2021 Apr 20.

Abstract

This review captures the anabolic and stimulatory effects observed with inhibition of the transforming growth factor β superfamily in muscle, blood, and bone. New medicinal substances that rectify activin, myostatin, and growth differentiation factor 11 signaling give hope to the many whose lives are affected by deterioration of these tissues. The review first covers the origin, structure, and common pathway of activins, myostatin, and growth differentiation factor 11 along with the pharmacodynamics of the new class of molecules designed to oppose the activin receptor signaling pathway. Current terminology surrounding this new class of molecules is inconsistent and does not infer functionality. Adopting inhibitors of the activin receptor signaling pathway (IASPs) as a generic term is proposed because it encapsulates the molecular mechanisms along the pathway trajectory. To conclude, a pragmatic classification of IASPs is presented that integrates functionality and side effects based on the data available from animals and humans. This provides researchers and clinicians with a tool to tailor IASPs therapy according to the need of projects or patients and with respect to side effects.

摘要

这篇综述总结了抑制转化生长因子-β 超家族在肌肉、血液和骨骼中产生的合成代谢和刺激作用。纠正激活素、肌肉生长抑制素和生长分化因子 11 信号的新药物有望为许多受这些组织恶化影响的人带来希望。该综述首先介绍了激活素、肌肉生长抑制素和生长分化因子 11 的起源、结构和常见途径,以及设计用于拮抗激活素受体信号通路的新型分子的药效学。目前围绕这一新类分子的术语并不一致,也不能推断其功能。提议将激活素受体信号通路抑制剂 (IASPs) 作为一个通用术语,因为它包含了沿途径轨迹的分子机制。最后,根据动物和人类的可用数据,提出了一个基于功能和副作用的 IASP 实用分类法,为研究人员和临床医生提供了根据项目或患者的需求以及副作用来定制 IASP 治疗的工具。

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