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A new strategy for the in vitro selection of stapled peptide inhibitors by mRNA display.

Emil S IqbalStacie L RichardsonNicolas A AbrigoKara K DodsH Estheban Osorio FrancoHeather S GerrishHari Kiran KotapatiIain M MorganDouglas S MastersonMatthew C T Hartman
Published in: Chemical communications (Cambridge, England) (2019)
Hydrocarbon stapled peptides are promising therapeutics for inhibition of intracellular protein-protein interactions. Here we develop a new high-throughput strategy for hydrocarbon stapled peptide discovery based on mRNA display of peptides containing α-methyl cysteine and cyclized with m-dibromoxylene. We focus on development of a peptide binder to the HPV16 E2 protein.
Keyphrases
  • high throughput
  • small molecule
  • amino acid
  • binding protein
  • single cell
  • fluorescent probe