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Tumor Discovery A comprehensive review of bexarotene
Figure 2. Schematic representation of bexarotene receptor binding results in the formation of RXR/NR dimer, leading to transcription initiation.
Abbreviations: NR: Nuclear receptor; RARE: Retinoic acid response elements; RXR: Retinoid X receptor.
3.3. Regulation of lipid metabolism affect the Wnt/β-catenin signaling pathway, which plays
Bexarotene has been shown to regulate lipid metabolism by a crucial role in cell proliferation and differentiation.
activating RXR receptors. It can increase the expression of Bexarotene has been found to modulate the expression of
lipid metabolism and transport genes, such as ATP-binding Wnt signaling components, suggesting potential crosstalk
[14]
cassette transporter A1 and apolipoprotein E. This effect of between bexarotene and this pathway .
bexarotene has been studied in the context of its potential 4. Distribution and accumulation
therapeutic role in disorders such as hyperlipidemia and
Alzheimer’s disease . Bexarotene gets distributed and accumulated in various
[12]
tissues throughout the body, a process influenced by
3.4. Interactions with co-regulatory proteins factors such as pharmacokinetics, metabolism, and specific
Bexarotene’s mechanism of action also involves interactions tissue characteristics. Depending on the conditions being
with co-regulatory proteins that modulate gene expression. treated, bexarotene is primarily administered either
These co-regulators can either enhance (co-activators) topically for CTCL or orally for other conditions. Topical
or suppress (co-repressors) the transcriptional activity of application allows for a higher concentration of bexarotene
RXR heterodimers. Examples of co-regulatory proteins in affected skin tissues, while oral administration enables
include steroid receptor coactivator-1 and nuclear receptor its distribution throughout the body. Bexarotene undergoes
corepressor . metabolism in the liver and excreted through bile,
[13]
facilitating its reach to different tissues. The concentrations
3.5. Crosstalk with other signaling pathways of bexarotene in these tissues are influenced by dosage,
Bexarotene can also interact with and influence other administration route, patient characteristics, and the type
signaling pathways. For example, it has been shown to of disease being treated. When applied topically, bexarotene
Volume 2 Issue 2 (2023) 3 https://doi.org/10.36922/td.0436

