Inhibition of low-density lipoprotein receptor degradation with a cyclic peptide that disrupts the homodimerization of IDOL E3 ubiquitin ligase

Eilidh K. Leitch, Nagarajan Elumalai, Maria Fridén‐Saxin, Göran Dahl, Paul Wan, Paul Clarkson, Eric Valeur, Garry Pairaudeau, Helen Boyd, Ali Tavassoli

Chemical Science · 2018 · 22 citations · 30 references

DOIFull text

Open access

Concepts

Abstract

-CFFLYT as the lead inhibitor, and improved its activity through the incorporation of non-natural amino acids. The activity of the optimized cyclic peptide was assessed in hepatic cells, with a dose-dependent increase in LDLR levels observed in the presence of our IDOL homodimerization inhibitor.

References

30