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Updated: May 10, 2025

Synthesis and Structure Determination of µ-Conotoxin PIIIA Isomers with Different Disulfide Connectivities
Published on: October 2, 2018
An Orthogonal Protection Strategy for the Synthesis of Conotoxins Containing Three Disulfide Bonds
Hengyu Zhang1,2, Lai Yue Chan3, Huanhuan Zhang1,2
1Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Abstract:
Disulfide bonds are crucial for stabilizing bioactive peptides such as conotoxins. We have developed a method for synthesizing conotoxins with three disulfide bonds using Mob, Trt, and Acm protection groups for regionally selective synthesis. This approach enabled the efficient synthesis of peptides with the desired disulfide bond connectivities independent of their sequences. Using our strategy, we synthesized five conotoxins, achieving yields of 20-30%. The results demonstrate the potential of our method for synthesizing complex peptides with multiple disulfide bonds.
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