FXR is a nuclear receptor that regulates bile, cholesterol homeostasis, lipid and glucose metabolism. It can regulate a variety of diseases, including cancer and cardiovascular disease. Studies have shown that the level of FXR expression is associated with the development of cancers (breast, lung, pancreatic and esophageal cancers). It regulates various cellular signaling pathways, such as EGFR/ERK, NF-κB, p38/MAPK, PI3K/AKT, Wnt/β-catenin, and JAK/STAT. FXR has high potential as a novel biomarker for cancer diagnosis, prognosis and treatment.

FXR agonist GW4064 is reported to inhibit cell proliferation caused by cancer, such as liver and colon cancer. GW4064 also activates FXR targets and FXR-related molecules such as SHP, MRP-2, IBABP, MDR proteins, solsolic carriers, aromatase, and GADD to induce apoptosis in breast cancer cells. In addition, FXR inhibitors have also played a significant role in the treatment of cancer, such as: DY268, trisubstituted pyrazolamide has shown antagonism to FXR, it may be effective in cholestasis and hypercholesterolemia. At present, The ICE has developed a relevant detection platform for FXR targets and completed an in vitro screening model for FXR targets drugs to help in the discovery of new drugs.

Key words:

Farnesoid X Receptor; Cholesterol homeostasis; GW4064; DY268; breast cancer; hypercholesteremia;

Present the data at the cellular level

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DOI: 10.3389/fphar.2020.01122