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Total synthesis of mambalgin‐1/2/3 by two‐segment hydrazide‐based native chemical ligation
Author(s) -
Lan Huan,
Wu Kun,
Zheng Yong,
Pan Man,
Huang YiChao,
Gao Shuai,
Zheng QingYun,
Zheng JiShen,
Li YiMing,
Xiao Bailong,
Liu Lei
Publication year - 2016
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.2868
Subject(s) - native chemical ligation , hydrazide , chemistry , ligation , chemical ligation , peptide , residue (chemistry) , combinatorial chemistry , disulfide bond , chemical synthesis , venom , reagent , biochemistry , stereochemistry , microbiology and biotechnology , biology , organic chemistry , in vitro
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.