Inhibition of low-density lipoprotein receptor degradation with a cyclic peptide that disrupts the homodimerization of IDOL E3 ubiquitin ligase
Abstract
A cyclic peptide IDOL homodimerization inhibitor identified from a genetically encoded SICLOPPS library is active in vitro and in cells.
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The first peptide-based IDOL inhibitor was recently reported.
“This makes IDOL an attractive target, and accordingly the first peptide-based IDOL inhibitor was recently reported [118].”
From The low-density lipoprotein receptor: Emerging post-transcriptional regulatory mechanisms (2025) · cites this paper as [118]
The experimental peptide-based IDOL inhibitor moderately increases LDLR abundance in cell models by disrupting IDOL dimerization.
“This experimental inhibitor moderately increases LDLR abundance in cell models by disrupting IDOL dimerization.”
From The low-density lipoprotein receptor: Emerging post-transcriptional regulatory mechanisms (2025) · cites this paper as [118]
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Production of cyclic peptides and proteins <i>in vivo</i>
Scott, C. P., Abel-Santos, E., Wall, M., Wahnon, D. C., & Benkovic, S. J. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.24.13638 · Cited by 402
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Sorted by citations
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
- Leitch, E. K., Elumalai, N., Fridén-Saxin, M., Dahl, G., Wan, P., Clarkson, P., Valeur, E., Pairaudeau, G., Boyd, H., & Tavassoli, A.
- Affiliations
- Chemistry
- Medicinal Chemistry
- Structure and Biophysics
- AstraZeneca
- Drug Safety and Metabolism
- ORCID
- Tavassoli, Ali
- Venue
- Chemical Science
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2018
- Volume
- 9
- Issue
- 27
- Pages
- 5957-5966
- ISSN
- 2041-6520
- 2041-6539
- PMC
- PMC6050537
- Cited by
- 25
- References
- 10
- Language
- en
- Funders
- AstraZeneca
- Engineering and Physical Sciences Research Council (EP/L505067/1)
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