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糜酶抑制剂的作用靶点。

Targets of chymase inhibitors.

机构信息

Osaka Medical College, Department of Pharmacology, Daigaku-machi 2-7, Takatsuki City, Osaka 569-8686, Japan.

出版信息

Expert Opin Ther Targets. 2011 Apr;15(4):519-27. doi: 10.1517/14728222.2011.555401. Epub 2011 Feb 4.

Abstract

INTRODUCTION

Chymase converts angiotensin I to angiotensin II and it can also convert precursors of TGF-β and MMP-9 to their active forms. Therefore, diseases related to angiotensin II TGF-β, and MMP-9 could potentially be treated with chymase inhibitors.

AREAS COVERED

This review discusses the appropriate targets and safety of chymase inhibitors. Six diseases with notable mortality or morbidity as targets of chymase inhibitors are focused on; abdominal aortic aneurysms (AAAs), nephropathy and retinopathy, cardiomyopathy, nonalcoholic steatohepatitis (NASH), organ fibrosis and intestinal diseases.

EXPERT OPINION

If chymase inhibition proves to be a useful strategy for the attenuation of angiotensin II, TGF-β and MMP-9 in vivo, the application of chymase inhibitors is likely to become widespread in various diseases in the clinical setting. Chymase inhibitors are anticipated not to interfere with the homeostasis of resting tissues, that is, those not affected by injury or inflammation.

摘要

简介

糜酶可将血管紧张素 I 转化为血管紧张素 II,还可将 TGF-β 和 MMP-9 的前体转化为其活性形式。因此,与血管紧张素 II、TGF-β 和 MMP-9 相关的疾病可能可以用糜酶抑制剂进行治疗。

涵盖领域

本文讨论了糜酶抑制剂的适当靶点和安全性。本文重点关注了六种死亡率或发病率较高的疾病作为糜酶抑制剂的靶点:腹主动脉瘤(AAA)、肾病和视网膜病变、心肌病、非酒精性脂肪性肝炎(NASH)、器官纤维化和肠道疾病。

专家意见

如果糜酶抑制被证明是体内抑制血管紧张素 II、TGF-β 和 MMP-9 的有效策略,那么糜酶抑制剂在临床环境中可能会广泛应用于各种疾病。糜酶抑制剂预计不会干扰静止组织的内稳平衡,即那些不受损伤或炎症影响的组织。

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