1. Total synthesis of mambalgin-1/2/3 by two-segment hydrazide-based native chemical ligation.
- Author
-
Lan H, Wu K, Zheng Y, Pan M, Huang YC, Gao S, Zheng QY, Zheng JS, Li YM, Xiao B, and Liu L
- Subjects
- Azides chemistry, Disulfides chemistry, Elapid Venoms chemistry, Models, Molecular, Molecular Structure, Peptides chemistry, Elapid Venoms chemical synthesis, Peptides chemical synthesis
- Abstract
Mambalgins are a class of 57-residue polypeptide toxins isolated from the venom of the African mamba. They exhibit potent analgesic effects by inhibiting the acid-sensing ion channels. Classified as members of the family of three-finger toxins, mambalgins contain four pairs of disulfide bridges that help to stabilize the three-finger scaffold. Here, we report the chemical synthesis of functional mambalgin-1/2/3 by using one-step two-segment hydrazide-based native chemical ligation. The two-segment ligation approach reported here may enable efficient production of mambalgin toxins. These synthetic mambalgins are useful compounds for development of diagnostic or therapeutic reagents. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd., (Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd.)
- Published
- 2016
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