scholarly journals The nuclear bile acid receptor FXR as a novel therapeutic target in cholestatic liver diseases: Hype or hope?

Hepatology ◽  
2004 ◽  
Vol 40 (1) ◽  
pp. 260-263 ◽  
Author(s):  
Michael Trauner
Keyword(s):  
Bile Acid ◽  
Therapeutic Target ◽  
Liver Diseases ◽  
Acid Receptor ◽  
Bile Acid Receptor ◽  
Novel Therapeutic

scholarly journals Bile Acid Receptor Therapeutics Effects on Chronic Liver Diseases

2020 ◽  
Vol 7 ◽  
Author(s):  
Vik Meadows ◽  
Lindsey Kennedy ◽  
Debjyoti Kundu ◽  
Gianfranco Alpini ◽  
Heather Francis
Keyword(s):  
Bile Acid ◽  
Liver Diseases ◽  
Chronic Liver ◽  
Chronic Liver Diseases ◽  
Acid Receptor ◽  
Bile Acid Receptor

scholarly journals MRGPRX4 is a bile acid receptor for human cholestatic itch

eLife ◽  
2019 ◽  
Vol 8 ◽  
Author(s):  
Huasheng Yu ◽  
Tianjun Zhao ◽  
Simin Liu ◽  
Qinxue Wu ◽  
Omar Johnson ◽  
...  
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Liver Diseases ◽  
Dorsal Root ◽  
Drug Target ◽  
Human Subjects ◽  
Acid Receptor ◽  
Chronic Itch ◽  
Natural Ligands ◽  
Bile Acid Receptor

Patients with liver diseases often suffer from chronic itch, yet the pruritogen(s) and receptor(s) remain largely elusive. Here, we identify bile acids as natural ligands for MRGPRX4. MRGPRX4 is expressed in human dorsal root ganglion (hDRG) neurons and co-expresses with itch receptor HRH1. Bile acids elicited Ca2+ responses in cultured hDRG neurons, and bile acids or a MRGPRX4 specific agonist induced itch in human subjects. However, a specific agonist for another bile acid receptor TGR5 failed to induce itch in human subjects and we find that human TGR5 is not expressed in hDRG neurons. Finally, we show positive correlation between cholestatic itch and plasma bile acids level in itchy patients and the elevated bile acids is sufficient to activate MRGPRX4. Taken together, our data strongly suggest that MRGPRX4 is a novel bile acid receptor that likely underlies cholestatic itch in human, providing a promising new drug target for anti-itch therapies.

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