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The Epigenetic Drug 5-Azacytidine Interferes with Cholesterol and Lipid Metabolism
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Several compounds known to increase LDLR mRNA stability directly have also been reported to decrease expression of SREBP-regulated genes, including PCSK9, exhibiting a dual effect.
“Interestingly, while these compounds are known to increase LDLR mRNA stability directly, several have also been reported to decrease the expression of SREBP-regulated genes, including PCSK9, thus exhibiting a dual effect that could have significant implications for cholesterol management [19,35,42].”
From The low-density lipoprotein receptor: Emerging post-transcriptional regulatory mechanisms (2025) · cites this paper as [42]
Triciribine shares with berberine and 5-AzaC the traits of inhibition of DNA synthesis, induction of ERK activity, stabilization of LDLR mRNA, and inhibition of PCSK9 expression.
“Interestingly, triciribine shares a number of similar traits with berberine and 5-AzaC: 1) inhibition of DNA synthesis, 2) induction of ERK activity, 3) stabilization of LDLR mRNA and 4) inhibition of PCSK9 expression11,34,35,49–51.”
From Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA (2018) · cites this paper as [35]
The effects of triciribine on LDLR mRNA stability and PCSK9 levels were reminiscent of those elicited by berberine and 5-Azacytidine (5-AzaC).
“The effects of triciribine on LDLR mRNA stability and PCSK9 levels were reminiscent of those elicited by berberine and 5-Azacytidine (5-AzaC)11,34,35.”
From Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA (2018) · cites this paper as [35]
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Sorted by citations
GRP94 Regulates Circulating Cholesterol Levels through Blockade of PCSK9-Induced LDLR Degradation
Poirier, S., Mamarbachi, M., Chen, W.-T., Lee, A. S., & Mayer, G. (2015) · Cell Reports · doi:10.1016/j.celrep.2015.11.006 · Cited by 86
Self-citationTriciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA
Bjune, K., Wierød, L., & Naderi, S. (2018) · Scientific Reports · doi:10.1038/s41598-018-34237-6 · Cited by 36
The low-density lipoprotein receptor: Emerging post-transcriptional regulatory mechanisms
Ndoj, K., Meurs, A., Papaioannou, D., Bjune, K., & Zelcer, N. (2025) · Atherosclerosis · doi:10.1016/j.atherosclerosis.2024.119082 · Cited by 17
Metadata
- Authors
- Poirier, S., Samami, S., Mamarbachi, M., Demers, A., Chang, T. Y., Vance, D. E., Hatch, G. M., & Mayer, G.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2014-07
- Volume
- 289
- Issue
- 27
- Pages
- 18736-18751
- ISSN
- 0021-9258
- Cited by
- 47
- References
- 2
- Language
- en
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