Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Mar Drugs
2022 Aug 12;208:. doi: 10.3390/md20080511.
Show Gene links
Show Anatomy links
Fluorescently Labeled α-Conotoxin TxID, a New Probe for α3β4 Neuronal Nicotinic Acetylcholine Receptors.
Huang M
,
Zhu X
,
Yang Y
,
Tan Y
,
Luo S
,
Zhangsun D
.
???displayArticle.abstract???
Neuronal nicotinic acetylcholine receptors (nAChRs) are important ion channel membrane proteins that are widely distributed in the central nervous system (CNS) and peripheral nervous system (PNS). As an important member, α3β4 nAChRs are related to pain sensation in PNS and nicotine addiction in CNS. However, research related to the α3β4 nAChRs is greatly limited by the lack of subtype-selective pharmacological tools. The α-conotoxin (α-CTx) TxID from the marine cone snail, Conus textile, is a selective α3β4 nAChR antagonist with relatively high potency. In this study, a fluorescent dye (5-TAMRA SE) was used to label TxID on the N-terminus of α-CTx TxID, and pure TxID-F (fluorescent analogue of TxID) was obtained by HPLC. At the same time, the potency and selectivity of TxID-F were detected by high-performance liquid chromatography (HPLC). Additionally, the potency and selectivity of TxID-F were determined by using a two-electrode voltage-clamp technique on various nAChRs expressed in the Xenopus oocyte expression system. The results obtained by electrophysiology showed that TxID-F maintained the same order of potency (IC50 73 nM) as the native toxin (IC50 25 nM) for the α3β4 nAChR subtype. In addition, the results of fluorescent spectroscopy and circular dichroism showed TxID-F has the same fluorescence as 5-TAMRA SE, as well as similar profiles as TxID. The results of flow cytometry showed that the histogram shifted significantly to the right for the RAW264.7 cells expressing α3β4-containing nAChRs stained with TxID-F and confirmed by live cell imaging. The study of fluorescent-labeled α-CTx TxID provides a rich pharmacological tool to explore the structure-function relationship, distribution, and ligand-binding domain of α3β4 nAChR subtype in the future.
Becchetti,
Nicotinic Receptors in Sleep-Related Hypermotor Epilepsy: Pathophysiology and Pharmacology.
2020, Pubmed
Becchetti,
Nicotinic Receptors in Sleep-Related Hypermotor Epilepsy: Pathophysiology and Pharmacology.
2020,
Pubmed
Brunzell,
Alpha7 nicotinic acetylcholine receptors modulate motivation to self-administer nicotine: implications for smoking and schizophrenia.
2012,
Pubmed
Chang,
Discovery of a potent and selective α3β4 nicotinic acetylcholine receptor antagonist from an α-conotoxin synthetic combinatorial library.
2014,
Pubmed
,
Xenbase
Davis,
Detection of fetal red cells in fetomaternal hemorrhage using a fetal hemoglobin monoclonal antibody by flow cytometry.
1998,
Pubmed
Eggan,
α3β4 nicotinic receptors in the medial habenula and substance P transmission in the interpeduncular nucleus modulate nicotine sensitization.
2017,
Pubmed
Fisher,
Cy3-RgIA-5727 Labels and Inhibits α9-Containing nAChRs of Cochlear Hair Cells.
2021,
Pubmed
,
Xenbase
Fölling,
Photochromic rhodamines provide nanoscopy with optical sectioning.
2007,
Pubmed
Ghimire,
Nicotinic Receptor Subunit Distribution in Auditory Cortex: Impact of Aging on Receptor Number and Function.
2020,
Pubmed
Giribaldi,
Backbone Cyclization Turns a Venom Peptide into a Stable and Equipotent Ligand at Both Muscle and Neuronal Nicotinic Receptors.
2020,
Pubmed
Glick,
Brain regions mediating α3β4 nicotinic antagonist effects of 18-MC on nicotine self-administration.
2011,
Pubmed
Guddat,
Three-dimensional structure of the alpha-conotoxin GI at 1.2 A resolution.
1996,
Pubmed
Hone,
A novel fluorescent alpha-conotoxin for the study of alpha7 nicotinic acetylcholine receptors.
2009,
Pubmed
,
Xenbase
Hone,
Alexa Fluor 546-ArIB[V11L;V16A] is a potent ligand for selectively labeling alpha 7 nicotinic acetylcholine receptors.
2010,
Pubmed
,
Xenbase
Jackson,
The α3β4* nicotinic acetylcholine receptor subtype mediates nicotine reward and physical nicotine withdrawal signs independently of the α5 subunit in the mouse.
2013,
Pubmed
Jin,
Conotoxins: Chemistry and Biology.
2019,
Pubmed
Jones,
Localization and mobility of omega-conotoxin-sensitive Ca2+ channels in hippocampal CA1 neurons.
1989,
Pubmed
Li,
α-Conotoxin TxID and [S9K]TxID, α3β4 nAChR Antagonists, Attenuate Expression and Reinstatement of Nicotine-Induced Conditioned Place Preference in Mice.
2020,
Pubmed
Luo,
Characterization of a novel α-conotoxin from conus textile that selectively targets α6/α3β2β3 nicotinic acetylcholine receptors.
2013,
Pubmed
,
Xenbase
Luo,
A novel α4/7-conotoxin LvIA from Conus lividus that selectively blocks α3β2 vs. α6/α3β2β3 nicotinic acetylcholine receptors.
2014,
Pubmed
,
Xenbase
Mashimo,
Regulation of Immune Functions by Non-Neuronal Acetylcholine (ACh) via Muscarinic and Nicotinic ACh Receptors.
2021,
Pubmed
McCallum,
α3β4 nicotinic acetylcholine receptors in the medial habenula modulate the mesolimbic dopaminergic response to acute nicotine in vivo.
2012,
Pubmed
Millar,
Diversity of vertebrate nicotinic acetylcholine receptors.
2009,
Pubmed
Moccia,
Expression and function of neuronal nicotinic ACh receptors in rat microvascular endothelial cells.
2004,
Pubmed
Muttenthaler,
On-resin strategy to label α-conotoxins: Cy5-RgIA, a potent α9α10 nicotinic acetylcholine receptor imaging probe.
2020,
Pubmed
,
Xenbase
Nicke,
Isolation, structure, and activity of GID, a novel alpha 4/7-conotoxin with an extended N-terminal sequence.
2003,
Pubmed
,
Xenbase
Paterson,
Neuronal nicotinic receptors in the human brain.
2000,
Pubmed
,
Xenbase
Pisani,
Targeting striatal cholinergic interneurons in Parkinson's disease: focus on metabotropic glutamate receptors.
2003,
Pubmed
Salas,
The alpha3 and beta4 nicotinic acetylcholine receptor subunits are necessary for nicotine-induced seizures and hypolocomotion in mice.
2004,
Pubmed
Sine,
Molecular dissection of subunit interfaces in the nicotinic acetylcholine receptor.
1998,
Pubmed
Sun,
α5-nAChR modulates nicotine-induced cell migration and invasion in A549 lung cancer cells.
2015,
Pubmed
Tan,
Inflammation Regulation via an Agonist and Antagonists of α7 Nicotinic Acetylcholine Receptors in RAW264.7 Macrophages.
2022,
Pubmed
Ulens,
Structural determinants of selective alpha-conotoxin binding to a nicotinic acetylcholine receptor homolog AChBP.
2006,
Pubmed
Vishwanath,
Synthesis of fluorescent analogs of alpha-conotoxin MII.
2006,
Pubmed
,
Xenbase
Wang,
Activation of α7 nAChR by PNU-282987 improves synaptic and cognitive functions through restoring the expression of synaptic-associated proteins and the CaM-CaMKII-CREB signaling pathway.
2020,
Pubmed
Wu,
α-Conotoxin [S9A]TxID Potently Discriminates between α3β4 and α6/α3β4 Nicotinic Acetylcholine Receptors.
2017,
Pubmed
,
Xenbase
Yang,
Design, Synthesis, and Activity of an α-Conotoxin LtIA Fluorescent Analogue.
2021,
Pubmed
,
Xenbase
Yoshikami,
The inhibitory effects of omega-conotoxins on Ca channels and synapses.
1989,
Pubmed
Zhangsun,
αO-Conotoxin GeXIVA disulfide bond isomers exhibit differential sensitivity for various nicotinic acetylcholine receptors but retain potency and selectivity for the human α9α10 subtype.
2017,
Pubmed
,
Xenbase
Zhilyakov,
Activation of Neuronal Nicotinic Receptors Inhibits Acetylcholine Release in the Neuromuscular Junction by Increasing Ca2+ Flux through Cav1 Channels.
2021,
Pubmed
Zoli,
Diversity of native nicotinic receptor subtypes in mammalian brain.
2015,
Pubmed
