Backbone-Cyclized Peptides

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Backbone cyclization is a technology which is used to make backbone cyclized peptides (BCPs). There are many chemical methods for implementing this technique, such as the solid-phase coherence strategy, the liquid phase coherence strategy and the natural chemical bonding within molecules and etc. Moreover, BCPs are cyclic peptides formed from the liner peptides through the cyclization between the C-terminal and the N-terminal. It is the cyclic structure between the head and tail makes the BCPs have good enzyme stability, thermal stability and chemical stability. And, parts of them have membrane permeability. Because of its abnormal stability and high biological activity, it has become a hot spot in the field of drug discovery, as well as the cyclization technology.

Application of Backbone-Cyclized Peptides

The natural function of the BCPs is host defense, that is, to protect the survival and continuation of this species by inhibiting the growth of alien organisms. Through the activity experiments, the researchers found that the BCPs also have some unique biological functions, which could be applied in treating human diseases. For example, the cyclotide in plants has the properties of uterine contractile activity, antimicrobial activity, anti-HIV activity and anti-tumor activity. However, the BCPs derived from organisms may be biotoxic to humans. In order to reduce the biotoxicity, the researchers will either mutate individual sites or fuse biologically active exogenous peptides into BCPs by “grafting”.

Available Services

Backbone-cyclized peptides are easily assembled via the formation of an amide bond between the peptides own N-terminus amine and C-terminus carboxylic acid. Our commonly used methods are chemical synthesis and biosynthesis. Creative Peptides perform the reaction with very high yields, and routinely provide over 98% purified cycled peptides. Our experienced scientists will tailor the most appropriate methods and 100% guaranteed service for customers. Every step of peptide synthesis is subject to Creative Peptides’ stringent quality control. Typical delivery specifications include:

  • HPLC chromatogram
  • Mass spec analysis
  • Synthesis report
  • Certificate of Analyses

References

  1. Zheng, J. S., Tang, S., Huang, Y. C., & Liu, L. (2013). Development of new thioester equivalents for protein chemical synthesis. Accounts of chemical research, 46(11), 2475-2484.
  2. Taichi, M., Hemu, X., Qiu, Y., & Tam, J. P. (2013). A thioethylalkylamido (TEA) thioester surrogate in the synthesis of a cyclic peptide via a tandem acyl shift. Organic letters, 15(11), 2620-2623.
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