Expression of CETP regulated by NR1H2 or NR1H3

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R-HSA-9035169
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Reaction [omitted]
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Homo sapiens
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The CETP gene is transcribed to yield mRNA and the mRNA is translated to yield protein. CETP expression can be transcriptionally activated by liver X receptors (LXRα (NR1H3) and LXRβ (NR1H2)) that belong to the nuclear receptor superfamily of ligand-activated transcription factors. Activation of NR1H2,3 induced expression via an LXR response element (LXRE) consisting of 2 hexanucleotide sequences separated by 4 intervening bases (an LXRE of the DR4 type) in the CETP promoter (Luo Y & Tall AR 2000), which may be more responsive to LXRα rather than LXRβ (Honzumi S et al. 2010). Treatment with T0901317, a synthetic agonist of NR1H2,3, increased CETP mRNA levels in human liver carcinoma HepG2 cells by approximately 220%, while NR1H3 silencing markedly diminished the increased expression of CETP (Shimada A et al. 2016). It should be noted that CETP is not expressed in the mouse or rat (it is a pseudogene in these species, Hogarth CA et al. 2003) so studies of LXR-mediated regulation of CETP have been performed in human, hamster, and non-human primates (Groot PHE, et al. 2005).

Literature References
PubMed ID Title Journal Year
20494359 LXRalpha regulates human CETP expression in vitro and in transgenic mice

Honzumi, S, Shima, A, Hiroshima, A, Koieyama, T, Ubukata, N, Terasaka, N

Atherosclerosis 2010
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