Date published: 2025-9-17

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BSEP Inhibitors

BSEP inhibitors constitute a distinctive chemical class characterized by their unique capability to interact with the Bile Salt Export Pump (BSEP), an integral protein localized within the hepatocyte cell membrane. These compounds modulate the function of BSEP, a vital component of the hepatobiliary transport system responsible for the efflux of bile salts into the bile canaliculus. By engaging with BSEP, these inhibitors can disrupt its normal function, thereby influencing the hepatobiliary transport of bile salts.

The significance of BSEP inhibitors lies in their ability to shed light on the intricate mechanisms governing hepatobiliary transport and bile salt homeostasis. Researchers have been actively investigating the precise molecular interactions between BSEP and these inhibitors, aiming to unravel the underlying molecular intricacies. This endeavor has led to the identification of diverse chemical structures within the BSEP inhibitor class, each possessing distinct molecular attributes that contribute to their binding affinity and impact on BSEP-mediated transport processes. The exploration of BSEP inhibitors not only advances our understanding of hepatic physiology but also holds broader implications for the intricate network of pathways involved in bile salt regulation. As researchers delve deeper into the mechanistic insights of BSEP inhibitors, they provide valuable contributions to the intricate puzzle of hepatobiliary transport, yielding insights into the intricate coordination of bile salt dynamics within the physiological context.

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