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Characterization of α-conotoxin TxIB and TxID for smoking cessation and drug rehabilitation

中国药理学与毒理学杂志 2018年第9期32卷 711-713页

作者： ZHANGSUN Dong-ting ZHU Xiao-peng ZHANGSUN Man-qi WU Yong LI Xiao-dan Sean CHRISTENSEN quentin kaas Peta J HARVEY David J CRAIK J Michael MCINTOSH LUO Su-lan Key Laboratory of Tropical Biological Resources of Ministry of Education Key Lab for Marine Drug of Haikou Hainan University Haikou570228 China Departments of Biology and Psychiatry University of Utah Salt Lake City Utah 84112 USA Instit

Nicotinic acetylcholine receptors(nAChRs) are widely distributed ligand gated ion channels throughout the peripheral and central nervous systems of *** are 16 different n AChR subunits,α1-α7,α9,α10 and β1-β4,as well as γ,δ,and ε,which assemble into pentamers to form different nAChR subtypes with distinct pharmacological properties in *** them α6β2*(*designates other possible subunit),α3β4 and α4β2 nAChR subtypes are potential therapeutic targets for the treatment of ***,various n AChR subtypes are very difficult to pharmacologically distinguish from each *** α6* n AChRs are expressed by dopaminergic neurons in the central nervous system,which modulate the release of dopamine and are believed to be important in mediating tobacco,morphine,cocaine and ethanol *** α3β4 nAChRs present in the medial habenula with important role in influencing nicotine *** of α3β4 nAChRs in the medial habenula decreased the dose of nicotine that rodents would ***,new antagonists of α6β2* or α3β4 nA ChR subtypes are of considerable interest,which would give strategies to selectively modulate α6β2* or α3β4 nA ChR *** characterized an α-conotoxin(α-CTx)TxIB with 16 amino acids and an α-CTx TxID with 15 amino acids from Conus *** sequence of TxIB is *** sequence of TxID is GCCSHPVCSAMSPIC with C-terminal amidation *** peptides with a Ⅰ-Ⅲ and Ⅱ-Ⅳ disulfide con-nectivity were chemically *** residues between Cys-Ⅱ and Cys-Ⅲ and Cys-Ⅲand Cys-Ⅳ of α-CTx are commonly referred to as loops 1 and 2,*** number of residues in each of these loops is used to further classify the α-*** TxIB is classified as a 4/7α-CTx,whereas the α-CTx TxIB has a 4/6 *** peptides were tested on rat nAChRs heterologously expressed in Xenopus laevis *** α-CTx TxIB blocked α6/α3β2β3 nAChR with an IC50 of 28 nmol·L^(-1),which showed little or no block of all th

关键词： acetylcholine receptors smokingcessation drug rehabilitation α-conotoxins

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A novel Hainan ConotoxinPotently Blocks a9alO Nicotinic Acetylcholine Receptors

A novel Hainan ConotoxinPotently Blocks a9alO Nicotinic Acet...

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第12届生物毒素研究及医药应用学术大会

作者： Sulan Luo Dongting Zhangsun Peta J.Harvey quentin kaas Yong Wu Xiaopeng Zhu Yuanyan Hu Xiaodan Li Victor Tsetlin Melissa McIntyre Cheryl Dowell James C.Baxter Keith S Elmslie David J.Craik J.Michael McIntosh Key Laboratory of Tropical Biological Resources Ministry of EducationKey Lab for Marine Drug of HaikouHainan University Institute for Molecular Bioscience The University of Queensland Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of Sciences George E.Wahlen Veterans Affairs Medical Center and Departments of Biology and Psychiatry University of Utah

The a9al0 nicotinic acetylcholine receptor(nAChR) subtype is a recently identified target for the development of breast cancer chemotherapeutics and analgesics,particularly to treat neuropathic ***/function analyses of antagonists of this subtype are therefore essential for the development of specific therapeutic *** we report that αO-conotoxinGeXIVA(GeXVLA) from *** native to Hainan,China is a potent and selective antagonist of theα9α10 nAChR *** signal sequence of GeXVLA has high similarity with the O1-gene conotoxin *** predicted mature peptide(GeXVLA) has four Cys residues and its three disulfide isomers were *** pharmacologically characterized Ol-superfamily peptides contain six Cys residues are calcium,sodium or potassium channel ***,GeXTVA did not inhibit calcium channels but antagonized nAChRs,most potently on the α9α10nAChR subtype with an IC of 3.8 *** block was voltage dependent and kinetic analysis of toxin dissociation indicated that the binding site of GeXTVA does not overlap with that of the competitive antagonist ***,the most active disulfide isomer of GeXTVA is the bead isomer,comprising,according to NMR analysis,two well-resolved but uncoupled disulfide restrained *** ribbon isomer is almost as potent but has a more rigid structure built around a short *** contrast to most a-conotoxins,the globular isomer is the least potent and has a flexible,multi-conformational *** reduced mechanical hyperalgesia in the rat chronic constriction injury model of neuropathic pain,but had no effect on motor performance,warranting its further investigation as a possible therapeutic *** displays unique structural properties among other Conus peptides and represents a novel template for molecules active against neuropathic pain.

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