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An Orthogonal Protection Strategy for the Synthesis of Conotoxins Containing Three Disulfide Bonds

Year: 2025
Type: article
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.
Source: Marine Drugs
DOI: 10.3390/md23040168
Authors: Hengyu Zhang, Lai Yue Chan, Huanhuan Zhang, Tao Jiang, David J. Craik, Wenqing Cai, Rilei Yu
Institutions: Qingdao National Laboratory for Marine Science and Technology, Ocean University of China, The University of Queensland, ARC Centre of Excellence for Innovations in Peptide and Protein Science, Institute for Molecular Bioscience, Shandong Academy of Pharmaceutical Sciences
Language: English
Open Access status: gold
Estimated APC paid: $3,499
Awards: G1573137754, G2064855699, G632657752, G6581110144, G8083103085, G8404384998
OpenAlex ID: W4409438681
FWCI: 1.01
Cites: 35
Cited by: 4
Related to: 10