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Design of New α-Conotoxins: From Computer Modeling to Synthesis of Potent Cholinergic Compounds
Mar. Drugs 2013, 11(9), 3537-3553; doi:10.3390/md11093537

Optimal Cleavage and Oxidative Folding of α-Conotoxin TxIB as a Therapeutic Candidate Peptide

*  and *
Key Laboratory of Tropical Biological Resources, Ministry of Education, Key Lab for Marine Drug of Haikou, Hainan University, Haikou, Hainan 570228, China
* Authors to whom correspondence should be addressed.
Received: 5 August 2013 / Revised: 16 August 2013 / Accepted: 19 August 2013 / Published: 17 September 2013
(This article belongs to the Special Issue Conotoxins)
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Alpha6beta2 nicotinic acetylcholine receptors (nAChRs) are potential therapeutic targets for the treatment of several neuropsychiatric diseases, including addiction and Parkinson’s disease. Alpha-conotoxin (α-CTx) TxIB is a uniquely selective ligand, which blocks α6/α3β2β3 nAChRs only, but does not block the other subtypes. Therefore, α-CTx TxIB is a valuable therapeutic candidate peptide. Synthesizing enough α-CTx TxIB with high yield production is required for conducting wide-range testing of its potential medicinal applications. The current study optimized the cleavage of synthesized α-CTx TxIB resin-bounded peptide and folding of the cleaved linear peptide. Key parameters influencing cleavage and oxidative folding of α-CTx TxIB were examined, such as buffer, redox agents, pH, salt, co-solvent and temperature. Twelve conditions were used for cleavage optimization. Fifty-four kinds of one-step oxidative solution were used to assess their effects on each α-CTx TxIB isomers’ yield. The result indicated that co-solvent choices were particularly important. Completely oxidative folding of globular isomer was achieved when the NH4HCO3 or Tris-HCl folding buffer at 4 °C contained 40% of co-solvent DMSO, and GSH:GSSG (2:1) or GSH only with pH 8~8.7.
Keywords: α-conotoxin TxIB; oxidative folding; optimization; therapeutic peptides α-conotoxin TxIB; oxidative folding; optimization; therapeutic peptides
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Wu, X.; Wu, Y.; Zhu, F.; Yang, Q.; Wu, Q.; Zhangsun, D.; Luo, S. Optimal Cleavage and Oxidative Folding of α-Conotoxin TxIB as a Therapeutic Candidate Peptide. Mar. Drugs 2013, 11, 3537-3553.

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