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Site-Specific Molecular Glues for the 14-3-3/Tau pS214 ProteinProtein Interaction via Reversible Covalent Imine Tethering

Covalent Modifiers

Using different biophysical assays, the stabilizing potency of the imine-bond forming molecules was mapped and X-ray crystallography studies provided structural data on the binding mode of the ternary complexes.

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Obstacles and innovations of macrocyclic drug development

Drug Target Review

11 Macrocycles can also be engineered in other ways to become more cell permeable; for example, by incorporating N-methyl groups in macrocyclic peptides. 12 Ring bridging strategies have also been effective in addressing permeability, as seen with MK-0616.