Peptide and peptide library cyclization via bromomethylbenzene derivatives.

@article{Hacker2015PeptideAP,
  title={Peptide and peptide library cyclization via bromomethylbenzene derivatives.},
  author={David E Hacker and Mohammed Almohaini and Aruna Anbazhagan and Zhong Ma and Matthew C T Hartman},
  journal={Methods in molecular biology},
  year={2015},
  volume={1248},
  pages={105-17}
}
Cyclization confers several advantages to peptides, cumulatively serving to make them more drug-like. In this protocol, cyclic peptides are generated via bis-alkylation of cysteine-containing peptides using α,α'-dibromo-m-xylene. The reactions are robust and high yielding. Multiple reaction platforms for the application of this versatile strategy are described herein: the cyclization of solid-phase-synthesized peptides, both in solution and on resin, as well as the cyclization of in vitro… CONTINUE READING
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