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The LXR-ApoE pathway was originally identified as a cancer target using a novel microRNA-based discovery platform developed by RGENIX’s scientific co-founders at The Rockefeller University.
RGX-104 (abequolixron) is an orally administered small molecule agonist of the Liver X Receptor (LXR) which activates expression of the APOE tumor suppressor protein.
Importantly, use of an LXR agonist to increase lipidated forms of ApoE in a mouse model of AD resulted in reduced Aβ plaque levels and an improvement in contextual memory.
In contrast, treatment with LXR or RXR ligands increases ABCA1 and apoE levels and significantly ameliorates amyloid pathology. In a recent study using APP mice we demonstrated that ABCA1 haplo ...
Mechanistically, LXR activation was shown to affect the survival of MDSCs, promoting their apoptosis in vitro and in mice. Studies using knockout mouse models revealed that APOE was mediating LXR ...
Importantly, use of an LXR agonist to increase lipidated forms of ApoE in a mouse model of AD resulted in reduced A? plaque levels and an improvement in contextual memory.
Receptors, including ApoE receptor 2 (see Part 1 of this three-part series), topped the hit parade of ApoE accomplices that might mediate nefarious actions of the risky isoform, ... (LXR) agonists.
After establishing that the intracellular protease neprilysin destroys Aβ42, they found that this destruction could be enhanced by adding ApoE to microglial cultures, or by inducing expression of ApoE ...
Cold exposure is shown to aggravate osteoarthritis (OA) by suppressing chondrocyte APOE, triggering lipid accumulation, ...
The authors concluded from these results that "distinct APOE genotypes elicited differential responsiveness to LXR agonistic therapy and might serve as potential genetic biomarkers for current ...
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