Anti-fibrotic Potential of AT2 Receptor Agonists

Frontiers in Pharmacology

Baydaa Hirmiz¹  Mark Del Borgo¹  Marie-Isabel Aguilar¹  Tracey A. Gaspari²  Robert E. Widdop²  Chrishan S. Samuel²  Huey W. Lee²  Yan Wang²  Dhaniel Baraldi²  Kate M. Denton³ 

[1] Department of Biochemistry and Molecular Biology, Cardiovascular Disease Program, Biomedicine Discovery Institute, Monash University, ClaytonVIC, Australia;Department of Pharmacology, Cardiovascular Disease Program, Biomedicine Discovery Institute, Monash University, ClaytonVIC, Australia;Department of Physiology, Cardiovascular Disease Program, Biomedicine Discovery Institute, Monash University, ClaytonVIC, Australia;

关键词: AT2 receptor;    compound 21;    cardiac fibrosis;    renal fibrosis;    inflammation;   

DOI  :  10.3389/fphar.2017.00564

来源: DOAJ

【 摘 要 】

There are a number of therapeutic targets to treat organ fibrosis that are under investigation in preclinical models. There is increasing evidence that stimulation of the angiotensin II type 2 receptor (AT2R) is a novel anti-fibrotic strategy and we have reviewed the published in vivo preclinical data relating to the effects of compound 21 (C21), which is the only nonpeptide AT2R agonist that is currently available for use in chronic preclinical studies. In particular, the differential influence of AT2R on extracellular matrix status in various preclinical fibrotic models is discussed. Collectively, these studies demonstrate that pharmacological AT2R stimulation using C21 decreases organ fibrosis, which has been most studied in the setting of cardiovascular and renal disease. In addition, AT2R-mediated anti-inflammatory effects may contribute to the beneficial AT2R-mediated anti-fibrotic effects seen in preclinical models.

【 授权许可】

Unknown