Solid Phase Peptide Synthesis (SPPS) allows for facile, expedient access to diverse libraries of peptide therapeutics. Through highly specified activity and complex functionality, these biologically relevant remedies have clear advantages over traditional small-molecule treatments. This investigation utilized on-resin SPPS to synthesize peptide therapeutics with distended backbones. Dimerization and thioacetal formation was then used to form highly-selective peptide antagonists of the EphA4 receptor that have been shown to slow the progression of neurodegeneration. In future experiments, high-throughput and efficient synthesis of diverse arrays of peptides through SPPS will be utilized to optimize macrocycle size in cyclic peptide therapeutics and engineer EphA4 antagonists with enhanced in vivo lifetimes.

On-resin solid-phase peptide synthesis of optimized peptide therapeutics

2019 Spring National Meeting

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