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Open AccessArticle

DSPE-PEG Modification of α-Conotoxin TxID

Key Laboratory of Tropical Biological Resources, Ministry of Education, Key Laboratory for Marine Drugs of Haikou, Hainan University, Haikou 570228, China
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Mar. Drugs 2019, 17(6), 342; https://doi.org/10.3390/md17060342
Received: 23 May 2019 / Accepted: 6 June 2019 / Published: 8 June 2019
In order to improve stability of a peptide marine drug lead, α-conotoxin TxID, we synthesized and modified TxID at the N-terminal with DSPE-PEG-NHS by a nucleophilic substitution reaction to prepare the DSPE-PEG-TxID for the first time. The reaction conditions, including solvent, ratio, pH, and reaction time, were optimized systematically and the optimal one was reacted in dimethyl formamide at pH 8.2 with triethylamine at room temperature for 120 h. The in vitro stabilities in serum, simulated gastric juice, and intestinal fluid were tested, and improved dramatically compared with TxID. The PEG-modified peptide was functionally tested on α3β4 nicotinic acetylcholine receptor (nAChR) heterologously expressed in Xenopus laevis oocytes. The DSPE-PEG-TxID showed an obvious inhibition effect on α3β4 nAChR. All in all, the PEG modification of TxID was improved in stability, resistance to enzymatic degradation, and may prolong the half-life in vivo, which may pave the way for the future application in smoking cessation and drug rehabilitation, as well as small cell lung cancer. View Full-Text
Keywords: α-conotoxin TxID; PEG modification; stability; α3β4 nAChR α-conotoxin TxID; PEG modification; stability; α3β4 nAChR
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Zhao, W.; Xiong, Y.; Zhangsun, D.; Luo, S. DSPE-PEG Modification of α-Conotoxin TxID. Mar. Drugs 2019, 17, 342.

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