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The **bile secretion pathway** is a complex physiological system involving hepatocellular uptake, intracellular transport, and canalicular excretion of bile acids, organic ions, phospholipids, cholesterol, and other substances. This network utilizes multiple membrane transporter proteins (such as BSEP, MDR3, NTCP, ASBT) and is regulated by hormones, nuclear receptors (e.g., FXR, PXR), signaling molecules, and the microbiota[1][2][3][4][5][6]. Modulation of this pathway is a therapeutic strategy for several metabolic and liver diseases by altering bile acid composition, pool size, signaling, or flow[2][4][6]. Pharmacological interventions focus on inhibiting specific transporters, activating or inhibiting nuclear or membrane receptors, or using bile acid derivatives to manage cholestasis, metabolic diseases, and associated complications.
Bile acid pool size reduction (via binding resins); Inhibition of bile acid transporters (e.g., ASBT, NTCP); Agonism/antagonism of bile acid receptors (FXR, TGR5); Alteration of bile acid composition; Stimulation of bile flow; Suppression of bile acid synthesis
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