Mechanism

FXR

Assets acting on this target.

Class
Farnesoid X receptor agonist

Farnesoid X receptor (FXR) is a nuclear receptor found mainly in liver and intestinal cells that acts as a sensor for bile acids, the cholesterol-derived molecules that aid fat digestion and also function as signaling messengers. When bile acids bind FXR, the receptor moves to the cell nucleus and changes the expression of genes that control how much new bile acid the liver makes, how bile acids are transported, and how the body handles lipids and glucose. Because bile acid buildup and disrupted lipid handling contribute to liver injury, synthetic FXR agonists are designed to recreate and amplify this natural feedback signal. This mechanism is of broad interest in chronic liver diseases marked by fat accumulation, inflammation, and scarring, as well as in cholestatic conditions where bile flow is impaired. By dampening bile acid production and improving downstream metabolic signaling, FXR activation is thought to reduce hepatic fat content, ease inflammatory and fibrotic processes, and improve aspects of glucose and lipid metabolism. As a nuclear receptor target, FXR is drugged with small molecules that can be taken orally and distributed to the liver and intestine, the tissues where the receptor is most physiologically active.

Research

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