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Tailored Cross‐β Assemblies to Establish the Peptides ‘Dominos’ for Anchoring the Undruggable Pharmacophores

Von Wiley-VCH zur Verfügung gestellt

β-sheet owns the ability to hierarchically stack into assemblies, and much effort has been made on designing different peptides to regulate their assembly behaviors. Although the progress is remarkable, it remains challenging to manipulate them in a controllable way for both tailored structures and specific active functions. In this study, we obtained bola-like peptides using de novo design and combinatorial chemical screening. By regulating the solvent accessible surface area of the peptide chain, a series of assemblies with different tilted angles and active sites of the β-sheet were obtained like collapsed ‘dominos’. The structure-activity relationship of the optimized peptide NQ40 system was established and its ability to target the PD-L1 was demonstrated. This study successfully established the structure-function relationship of β-sheets assemblies and has positive implications on rational design of the peptide assemblies to possess recognition abilities.

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