Helix stapled peptide
Arg-Ser-Gly-Pro-Pro-Gly-{S-α-(4’-pentenyl-alanine)}-Gln-Gly-Arg- {S-α-(4’-pentenyl-alanine)}-Gln-Arg-Leu-Leu-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2
Helix stabilisation by cross-linking is a relatively new approach enabling the design of highly selective peptides. To minimise the amount of expensive Verdine building blocks used for Ring-closing metathesis, 40µmol of peptidyl-resin was treated with Grub’s catalyst. Careful control of the quality of the peptide before and during stapling enabled the preparation of stapled Orexin B in excellent yield.
