This investigation uncovers how bi-triazine cross-linkers influence peptide conformation and biological activity, suggesting pathways for therapeutic advancements.
Key Points
The aim is to link cross-linker geometry with peptide conformation and biological performance.
Utilized eight bi-triazine cross-linkers with varying geometries
Studied cyclic RGD and dimeric KTLLPTP peptides as models
Conducted binding assays and cellular studies
Employed in vivo Ga-PET/CT imaging for evaluation
Identified lead candidate [68Ga]Ga-8a with ∼5 %ID/mL tumor contrast
In cyclic peptides, aromaticity and symmetry were crucial for binding
For dimeric peptides, bond length and angle improved binding via the 'molecular ruler' effect