Abstract
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 (AT2 R) 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 AT2 R agonist that is currently available for use in chronic preclinical studies. In particular, the differential influence of AT2 R on extracellular matrix status in various preclinical fibrotic models is discussed. Collectively, these studies demonstrate that pharmacological AT2 R stimulation using C21 decreases organ fibrosis, which has been most studied in the setting of cardiovascular and renal disease. In addition, AT2 R-mediated anti-inflammatory effects may contribute to the beneficial AT2 R-mediated anti-fibrotic effects seen in preclinical models.
| Original language | English |
|---|---|
| Article number | 564 |
| Number of pages | 7 |
| Journal | Frontiers in Pharmacology |
| Volume | 8 |
| DOIs | |
| Publication status | Published - 31 Aug 2017 |
Keywords
- AT receptor
- Cardiac fibrosis
- Compound 21
- Inflammation
- Renal fibrosis
Cite this
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Anti-fibrotic potential of AT2 receptor agonists. / Wang, Yan; Del Borgo, Mark; Lee, Huey W.; Baraldi, Dhaniel; Hirmiz, Baydaa; Gaspari, Tracey A.; Denton, Kate M.; Aguilar, Marie-Isabel; Samuel, Chrishan S.; Widdop, Robert E.
In: Frontiers in Pharmacology, Vol. 8, 564, 31.08.2017.Research output: Contribution to journal › Article › Other › peer-review
TY - JOUR
T1 - Anti-fibrotic potential of AT2 receptor agonists
AU - Wang, Yan
AU - Del Borgo, Mark
AU - Lee, Huey W.
AU - Baraldi, Dhaniel
AU - Hirmiz, Baydaa
AU - Gaspari, Tracey A.
AU - Denton, Kate M.
AU - Aguilar, Marie-Isabel
AU - Samuel, Chrishan S.
AU - Widdop, Robert E.
PY - 2017/8/31
Y1 - 2017/8/31
N2 - 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 (AT2 R) 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 AT2 R agonist that is currently available for use in chronic preclinical studies. In particular, the differential influence of AT2 R on extracellular matrix status in various preclinical fibrotic models is discussed. Collectively, these studies demonstrate that pharmacological AT2 R stimulation using C21 decreases organ fibrosis, which has been most studied in the setting of cardiovascular and renal disease. In addition, AT2 R-mediated anti-inflammatory effects may contribute to the beneficial AT2 R-mediated anti-fibrotic effects seen in preclinical models.
AB - 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 (AT2 R) 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 AT2 R agonist that is currently available for use in chronic preclinical studies. In particular, the differential influence of AT2 R on extracellular matrix status in various preclinical fibrotic models is discussed. Collectively, these studies demonstrate that pharmacological AT2 R stimulation using C21 decreases organ fibrosis, which has been most studied in the setting of cardiovascular and renal disease. In addition, AT2 R-mediated anti-inflammatory effects may contribute to the beneficial AT2 R-mediated anti-fibrotic effects seen in preclinical models.
KW - AT receptor
KW - Cardiac fibrosis
KW - Compound 21
KW - Inflammation
KW - Renal fibrosis
UR - http://www.scopus.com/inward/record.url?scp=85028471491&partnerID=8YFLogxK
U2 - 10.3389/fphar.2017.00564
DO - 10.3389/fphar.2017.00564
M3 - Article
VL - 8
JO - Frontiers in Pharmacology
JF - Frontiers in Pharmacology
SN - 1663-9812
M1 - 564
ER -