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. Author manuscript; available in PMC: 2020 Jul 14.
Published in final edited form as: J Am Chem Soc. 2020 Feb 4;142(7):3351–3355. doi: 10.1021/jacs.9b13405

Figure 1. Design of inhibitors that mimic the transmembrane domain of γ-secretase substrates.

Figure 1.

Helical peptide inhibitors (HPIs) directed to the substrate docking exosite were conjugated through a variable linker to transition-state analogue inhibitors (TSAs) directed to the active site. Presenilin (blue-grey) and other components of the γ-secretase complex (outlined) are shown schematically in the absence and presence of a hybrid HPI-TSA inhibitor.