Chemical Science · 2018 · 22 citations · 30 references
Life SciencesBiochemistryMolecular BiologyDrug DiscoveryLead OptimizationProtein-protein InteractionsEnzyme InhibitionHit-to-lead OptimizationLipoprotein MetabolismPeptide Drug DiscoveryProtein DegradationProtein-lipid InteractionsCyclic Peptide LibrariesCyclic PeptidesCyclized PeptidesLipoprotein ReceptorsPeptide Lead DiscoveryPeptide Lead OptimizationRegulation By E3 Ubiquitin LigasesUbiquitin Binding
-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.
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