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Open AccessArticle

Effects of Cyclization on Activity and Stability of α-Conotoxin TxIB

1
Key Laboratory of Tropical Biological Resources of Ministry of Education, Key Laboratory for Marine Drugs of Haikou, School of Life and Pharmaceutical Sciences, Hainan University, Haikou 570228, China
2
Medical School, Guangxi University, Nanning 530004, China
*
Authors to whom correspondence should be addressed.
Mar. Drugs 2020, 18(4), 180; https://doi.org/10.3390/md18040180
Received: 21 February 2020 / Revised: 25 March 2020 / Accepted: 25 March 2020 / Published: 29 March 2020
(This article belongs to the Special Issue Cone Snail Venom Peptides, from Treasure Hunt to Drug Leads)
α-Conotoxin TxIB specifically blocked α6/α3β2β3 acetylcholine receptors (nAChRs), and it could be a potential probe for studying addiction and other diseases related to α6/α3β2β3 nAChRs. However, as a peptide, TxIB may suffer from low stability, short half-life, and poor bioavailability. In this study, cyclization of TxIB was used to improve its stability. Four cyclic mutants of TxIB (cTxIB) were synthesized, and the inhibition of these analogues on α6/α3β2β3 nAChRs as well as their stability in human serum were measured. All cyclized analogues had similar activity compared to wild-type TxIB, which indicated that backbone cyclization of TxIB had no significant effect on its activity. Cyclization of TxIB with a seven-residue linker improved its stability significantly in human serum. Besides this, the results showed that cyclization maintained the activity of α-conotoxin TxIB, which is conducive to its future application. View Full-Text
Keywords: α-conotoxin TxIB; α6/α3β2β3 nAChRs; cyclization; activity; stability α-conotoxin TxIB; α6/α3β2β3 nAChRs; cyclization; activity; stability
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MDPI and ACS Style

Li, X.; Wang, S.; Zhu, X.; Zhangsun, D.; Wu, Y.; Luo, S. Effects of Cyclization on Activity and Stability of α-Conotoxin TxIB. Mar. Drugs 2020, 18, 180.

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