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This protocol provides a detailed procedure for the preparation of stapled ??-helical peptides, which have proven their potential as useful molecular probes and as next-generation therapeutics. Two crucial features of this protocol are (i) the construction of peptide substrates containing hindered ??-methyl, ??-alkenyl amino acids and (ii) the ring-closing olefin metathesis (RCM) of the resulting resin-bound peptide substrates. The stapling systems described in this protocol, namely bridging one or two turns of an ??-helix, are highly adaptable to most peptide sequences, resulting in favorable RCM kinetics, helix stabilization and promotion of cellular uptake.

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Bird, G. H.; Mazzola, E.; Opoku-Nsiah, K.; Lammert, M. A.; Godes, M.; Neuberg, D. S.; Walensky, L. D. Nat. Chem. Biol. 2016, 12, 845.Stapled peptides are an application of olefin metathesis first demonstrated by Grubbs and Blackwell1 using o-allyl amino acids,...