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凝血因子 Xa 作为一个新兴的药物靶点。

Blood coagulation factor Xa as an emerging drug target.

机构信息

Center for Experimental and Molecular Medicine, Academic Medical Center, Meibergdreef 9, NL-1105 AZ, Amsterdam, The Netherlands.

出版信息

Expert Opin Ther Targets. 2011 Mar;15(3):341-9. doi: 10.1517/14728222.2011.553608. Epub 2011 Jan 21.

Abstract

INTRODUCTION

Factor (F)Xa is well-known as an important player in the coagulation cascade responsible for thrombin generation. More recently, FXa emerged as an essential player in cell biology via activation of protease-activated receptors (PAR)-1 and -2. This pleiotropic role of FXa forms the basis for its potential contribution to the pathogenesis of several diseases.

AREAS COVERED

The role of FXa in pathophysiology is reviewed with special emphasis on its signal transduction properties. To this end, we first discuss the important role of FXa in the coagulation cascade, we continue with recent data on FXa induced signaling in pathophysiology with special emphasis on tissue remodeling and fibrosis and discuss the potential of FXa as an emerging drug target.

EXPERT OPINION

FXa is more than a passive intermediate in the coagulation cascade and FXa may in fact orchestrate fundamental processes during pathophysiology. Targeting FXa may be an exciting new therapeutic strategy in the treatment of (fibro)proliferative diseases for which current treatment options are limited.

摘要

简介

因子 (F)Xa 作为凝血级联反应中凝血酶生成的重要参与者而广为人知。最近,FXa 通过激活蛋白酶激活受体 (PAR)-1 和 -2,成为细胞生物学中的重要参与者。FXa 的这种多效性作用为其在多种疾病发病机制中的潜在作用奠定了基础。

涵盖领域

本文特别强调 FXa 的信号转导特性,综述了 FXa 在病理生理学中的作用。为此,我们首先讨论了 FXa 在凝血级联反应中的重要作用,然后继续讨论了 FXa 在病理生理学中诱导信号的最新数据,特别强调了组织重塑和纤维化,并讨论了 FXa 作为新兴药物靶点的潜力。

专家意见

FXa 不仅仅是凝血级联反应中的一个被动中间产物,实际上,FXa 可能在病理生理学过程中协调基本过程。针对 FXa 可能是一种治疗(纤维)增生性疾病的令人兴奋的新治疗策略,因为目前的治疗选择有限。

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