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RXR targeting holds therapeutic potential in cardiovascular disease but remains limited by toxicity.
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Review outlines the cardioprotective and metabolic functions of retinoid X receptors in the heart, highlighting their therapeutic potential despite current toxicity limits.
Retinoid X receptors (RXRs) are members of ligand-dependent transcription factors whose effects on a diversity of cellular processes, including cellular proliferation, the immune response, and lipid and glucose metabolism. Knock out of RXRα causes a hypoplasia of the myocardium which is lethal during fetal life. In addition, the heart maintains a well-orchestrated balances in utilizing fatty acids (FAs) and other substrates to meet the high energy requirements. As the master transcriptional regulators of lipid metabolism, RXRs become particularly important for the energy needs of the heart. Accumulating evidence suggested that RXRs may exert direct beneficial effects in the heart both through heterodimerization with other nuclear receptors (NRs) and homodimerization, thus standing as suitable targets for treating in cardiovascular diseases. Although compounds that target RXRs are promising drugs, their use is limited by toxicity. A better understanding of the structural biology of RXRs in cardiovascular disease should enable the rational design of more selective nuclear receptor modulators to overcome these problems. Here, this review summarizes a brief overview of RXRs structure and versatility of RXR action in the control of cardiovascular diseases. And we also discussed the therapeutic potential of RXR ligand.
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Shao et al. (2021) conducted a review in Cardiovascular diseases. Retinoid X receptor (RXR) modulators/ligands was evaluated. Retinoid X receptors (RXRs) regulate cardiac lipid metabolism and offer therapeutic potential in cardiovascular diseases, though RXR-targeting compounds are currently limited by toxicity.
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