Pro-apoptosis bicyclic polypeptide with stable alpha-helical conformation and a preparation method and application thereof
A technology of helical conformation and apoptosis, applied in the field of pro-apoptotic bicyclic polypeptides and preparation, can solve the problems of weak targeting, low cell penetration ability, poor metabolic stability of polypeptides, etc., and achieves a high degree of α-helix, Improved cyclization efficiency, small effect of normal cell killing ability
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Embodiment 1
[0043] This example provides a pro-apoptotic bicyclic polypeptide with a stable α-helical conformation, comprising a pro-apoptotic peptide functional peptide segment, targeting α v beta 3 Integrin RGD, turn-angle amino acid proline, and thioether-containing molecular backbone, the sequence of the pro-apoptotic peptide functional peptide is KLAKLXKKLAKLKK, which is a linear sequence rich in lysine, and X is a non- The natural amino acid, the pro-apoptotic peptide functional peptide and RGD are connected by proline to reduce the mutual interference between the pro-apoptotic peptide and RGD, and at the same time, it is convenient to turn into a loop and improve the flexibility of the connection. Acids construct bicyclic structures with thioether backbones on linear polypeptides through thiol-alkyne click chemistry reactions.
[0044] The amino acids in the sequence of the pro-apoptotic peptide functional peptide are all L-type amino acids, and have an α-helical conformation, whi...
Embodiment 2
[0056] This example provides a method for preparing a pro-apoptotic bicyclic polypeptide with stable α-helical conformation, as shown in the attached figure 1 As shown, the specific preparation process is as follows:
[0057] S1. Synthesize the linear peptide sequence Fmoc-WRGDfVPKLAKLXKKLAKLK(Alloc)K-Resin containing the allyloxycarbonyl Alloc side chain protection group by Fmoc solid-phase synthesis method, wherein the Alloc side chain protection group is located at the lysine on the right side of the sequence On the above, X is an unnatural amino acid with an alkyne group, and tryptophan is connected to the end of RGD. Tryptophan has an absorption peak at 280nm, and the concentration of the polypeptide can be determined by a microplate reader. The linear peptide sequence Fmoc-WRGDfVPKLAKLXKKLAKLK(Alloc) The specific structure of K-Resin is as follows:
[0058]
[0059] The specific synthesis process is as follows:
[0060] First weigh 400mg of Rink resin, swell it with...
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