Date published: 2025-9-16

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ABCG5 Activators

ABCG5 Activators represent a diverse class of molecules intricately connected to lipid and cholesterol metabolism. Their underlying influence on ABCG5, either direct or indirect, predominantly hinges on the regulation of sterol homeostasis. Agonists of liver X receptors (LXRs), such as GW3965 and T0901317, wield a definitive role in this realm. LXRs, being nuclear receptors, when activated, prompt a transcriptional response that favors the upregulation of genes associated with cholesterol efflux, including ABCG5. As part of the concerted action to ensure cholesterol balance, bile acids like Cholic acid and Ursodeoxycholic acid act as signaling molecules. Their presence and metabolism, especially with the involvement of Farnesoid X receptors (FXR), can shape the cellular response leading to modulation of ABCG5 expression.

Furthermore, components directly involved in cholesterol and lipid synthesis or metabolism, such as Desmosterol, Geranylgeraniol, or even exogenous agents like Fenofibrate and Rosiglitazone, interact with lipid homeostasis pathways. These pathways, while not exclusively targeting ABCG5, encapsulate a broad spectrum of proteins and processes that collaborate to maintain cellular sterol balance. Notably, fatty acids like Eicosapentaenoic acid (EPA) emphasize the broader landscape of lipid regulation and its interplay with ABCG5 function.

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