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  • Synthesis of all-hydrocarbon stapled α-helical peptides by ring-closing olefin metathesis.

Synthesis of all-hydrocarbon stapled α-helical peptides by ring-closing olefin metathesis.

Nature protocols (2011-06-04)
Young-Woo Kim, Tom N Grossmann, Gregory L Verdine
摘要

This protocol provides a detailed procedure for the preparation of stapled α-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 α-methyl, α-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 α-helix, are highly adaptable to most peptide sequences, resulting in favorable RCM kinetics, helix stabilization and promotion of cellular uptake.

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Sigma-Aldrich
Grubbs Catalyst® M102, Umicore, 97%
Sigma-Aldrich
Fmoc-( S )-2-(4-戊烯基)Ala-OH, ≥97%
Sigma-Aldrich
Fmoc-(R)-2-(7-octenyl)Ala-OH