What is the role of Riccardin C (RC) in modulating the activity of Liver X Receptors (LXRs)?

Label:chem

Topic
Riccardin C (RC) is a non-sterol natural product isolated from the liverwort Blasia pusilla. Liver X Receptors (LXRs) α and β are nuclear receptors that play critical roles in maintaining lipid homeostasis by regulating genes involved in cholesterol efflux, transport, and excretion.
Answer
Riccardin C functions as an LXRα agonist and an LXRβ antagonist. It binds directly to LXRα and recruits the coactivator SRC-1 peptide, leading to the activation of LXRα-dependent gene transcription. However, it fails to recruit a coactivator to LXRβ, resulting in the inhibition of LXRβ-mediated transactivation. This selective activity makes RC a potential tool for studying subtype-specific functions of LXRs and for developing therapeutic agents that target LXR pathways.
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