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Genomes and Genes | N S MillarSummaryAffiliation: University College London Country: UK Publications
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Publications
Activation of α7 nicotinic receptors by orthosteric and allosteric agonists: influence on single-channel kinetics and conductanceMagda M Pałczyńska
Department of Neuroscience, Physiology and Pharmacology, University College London, London, United Kingdom
Mol Pharmacol 82:910-7. 2012..3 ± 2.4 pS) than when activated by ACh (90.0 ± 2.7 pS), providing evidence that activation by allosteric and orthosteric agonists results in different α7 nAChRs open-channel conformations...
The Drosophila nicotinic acetylcholine receptor subunits Dα5 and Dα7 form functional homomeric and heteromeric ion channelsStuart J Lansdell
Department of Neuroscience, Physiology and Pharmacology, University College London, London, UK
BMC Neurosci 13:73. 2012..The focus of the present study is the Dα5, Dα6 and Dα7 subunits, which are distinguished by their sequence similarity to one another and also by their close similarity to the vertebrate α7 nAChR subunit...
A series of α7 nicotinic acetylcholine receptor allosteric modulators with close chemical similarity but diverse pharmacological propertiesJaskiran K Gill
Department of Neuroscience, Physiology and Pharmacology, University College London, London, UK
Mol Pharmacol 81:710-8. 2012..These findings provide evidence of the pharmacological diversity of compounds interacting with the allosteric transmembrane site on α7 nAChRs...
Competitive binding at a nicotinic receptor transmembrane site of two α7-selective positive allosteric modulators with differing effects on agonist-evoked desensitizationToby Collins
Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London, WC1E 6BT, United Kingdom
Neuropharmacology 61:1306-13. 2011..These data, together with computer docking simulations, lead us to conclude that both the type I PAM NS1738 and the type II PAM PNU-120596 bind competitively at a mutually exclusive intrasubunit transmembrane site...
Nicotinic acetylcholine receptors: targets for commercially important insecticidesNeil S Millar
Department of Pharmacology, University College London, Gower Street, London, WC1E 6BT, UK
Invert Neurosci 7:53-66. 2007..As with other classes of insecticides, there is growing evidence for the evolution of resistance to insecticides that act on nAChRs...
RIC-3: a nicotinic acetylcholine receptor chaperoneN S Millar
Department of Pharmacology, University College London, London, UK
Br J Pharmacol 153:S177-83. 2008..This review provides a brief history of RIC-3; from the identification of the ric-3 gene in C. elegans in 1995 to the more recent demonstration of its activity as a nAChR chaperone...
Assembly and trafficking of nicotinic acetylcholine receptors (Review)Neil S Millar
Department of Pharmacology, University College London, London, UK
Mol Membr Biol 25:279-92. 2008..This review will discuss nAChR subunit diversity and factors influencing receptor assembly and trafficking...
Diversity of vertebrate nicotinic acetylcholine receptorsNeil S Millar
Department of Neuroscience, Physiology and Pharmacology, University College London, London WC1E 6BT, UK
Neuropharmacology 56:237-46. 2009..This review will focus on vertebrate nAChRs and will provide an overview of the extent of nAChR diversity based on studies of both native and recombinant nAChRs...
A review of experimental techniques used for the heterologous expression of nicotinic acetylcholine receptorsNeil S Millar
Department of Neuroscience, Physiology and Pharmacology, University College London, London WC1E 6BT, UK
Biochem Pharmacol 78:766-76. 2009..It will focus, in particular, upon studies of recombinant nAChRs, work that has been conducted by many hundreds of scientists during a period of almost 30 years since the molecular cloning of nAChR subunits in the early 1980s...
Assembly and subunit diversity of nicotinic acetylcholine receptorsN S Millar
Department of Pharmacology, University College London, Gower Street, London WC1E 6BT, UK
Biochem Soc Trans 31:869-74. 2003..In this paper the extent of nAChR subunit diversity and evidence for receptor subunit composition is reviewed...
Characterisation of insect nicotinic acetylcholine receptors by heterologous expressionNeil S Millar
Department of Neuroscience, Physiology and Pharmacology, University College London, London, WC1E 6BT, UK
Adv Exp Med Biol 683:65-73. 2010..These approaches include the expression of hybrid nAChRs (containing insect nAChR subunit co-expressed with vertebrate subunits), artificial subunit chimeras and the co-expression of molecular chaperones such as RIC-3...
The influence of nicotinic receptor subunit composition upon agonist, alpha-bungarotoxin and insecticide (imidacloprid) binding affinityS J Lansdell
Department of Pharmacology, University College London, UK
Neuropharmacology 39:671-9. 2000..Our results demonstrate that both alpha and non-alpha subunits exert a profound influence upon the affinity of nicotinic ligands for recombinant nAChRs...
Cloning and heterologous expression of Dalpha4, a Drosophila neuronal nicotinic acetylcholine receptor subunit: identification of an alternative exon influencing the efficiency of subunit assemblyS J Lansdell
Department of Pharmacology, University College London, Gower Street, WC1E 6BT, London, UK
Neuropharmacology 39:2604-14. 2000..The relationship between Dalpha4 and other previously cloned nAChR subunits has been examined and the implications for the nomenclature of insect nAChRs is discussed...
Influence of the M3-M4 intracellular domain upon nicotinic acetylcholine receptor assembly, targeting and functionS Kracun
Department of Pharmacology, University College London, London, UK
Br J Pharmacol 153:1474-84. 2008..The aim of this study was to investigate the influence of the intracellular domain of nicotinic acetylcholine receptor (nAChR) subunits upon receptor assembly, targeting and functional properties...
Up-regulation of cell-surface alpha4beta2 neuronal nicotinic receptors by lower temperature and expression of chimeric subunitsS T Cooper
Wellcome Laboratory for Molecular Pharmacology, Department of Pharmacology, University College London, London WC1E 6BT, United Kingdom
J Biol Chem 274:27145-52. 1999....
Inefficient cell-surface expression of hybrid complexes formed by the co-assembly of neuronal nicotinic acetylcholine receptor and serotonin receptor subunitsP C Harkness
Department of Pharmacology, University College London, London WC1E 6BT, UK
Neuropharmacology 41:79-87. 2001....
Identification of domains influencing assembly and ion channel properties in alpha 7 nicotinic receptor and 5-HT3 receptor subunit chimaerasV J Gee
Department of Pharmacology, University College London, London, UK
Br J Pharmacol 152:501-12. 2007..With the aim of identifying the influence of subunit domains upon receptor assembly and function, a series of chimaeras have been constructed containing regions of the neuronal nAChR alpha 7 subunit and the 5-HT(3) receptor (3A) subunit...
The increased trafficking of the calcium channel subunit alpha2delta-1 to presynaptic terminals in neuropathic pain is inhibited by the alpha2delta ligand pregabalinClaudia S Bauer
Department of Neuroscience, Physiology and Pharmacology, University College London, London WC1E 6BT, United Kingdom
J Neurosci 29:4076-88. 2009....
A nicotinic acetylcholine receptor mutation (Y151S) causes reduced agonist potency to a range of neonicotinoid insecticidesZewen Liu
Department of Pharmacology, University College London, UK
J Neurochem 99:1273-81. 2006..3 to 3.6-fold). The relationship between neonicotinoid structure and their potency on nAChRs containing the Y151S target-site mutation is discussed...
Changes in conformation and subcellular distribution of alpha4beta2 nicotinic acetylcholine receptors revealed by chronic nicotine treatment and expression of subunit chimerasPatricia C Harkness
Department of Pharmacology, University College London, London, WC1E 6BT, United Kingdom
J Neurosci 22:10172-81. 2002..The finding that subunit conformation can be influenced by coassembled subunit partners is in agreement with models of receptor assembly which propose that subunit folding continues after initial subunit-subunit interactions...
Species selectivity of a nicotinic acetylcholine receptor agonist is conferred by two adjacent extracellular beta4 amino acids that are implicated in the coupling of binding to channel gatingGareth T Young
Department of Pharmacology, University College London, Gower Street, London, WC1E 6BT, UK
Mol Pharmacol 71:389-97. 2007..Our experimental data, together with homology models of the rat and human alpha3beta4 nAChRs, suggest that amino acids 55 and 56 may be involved in the coupling of agonist binding and channel gating...
Dbeta3, an atypical nicotinic acetylcholine receptor subunit from Drosophila : molecular cloning, heterologous expression and coassemblyStuart J Lansdell
Department of Pharmacology, University College London, London, UK
J Neurochem 80:1009-18. 2002....
Molecular characterization of Dalpha6 and Dalpha7 nicotinic acetylcholine receptor subunits from Drosophila: formation of a high-affinity alpha-bungarotoxin binding site revealed by expression of subunit chimerasStuart J Lansdell
Department of Pharmacology, University College London, London, UK
J Neurochem 90:479-89. 2004..In addition to the formation of homomeric nAChR complexes, evidence has been obtained from both radioligand binding and co-immunoprecipitation studies for the co-assembly of Dalpha6 and Dalpha7 into heteromeric cell surface complexes...
Temperature-sensitive expression of Drosophila neuronal nicotinic acetylcholine receptorsS J Lansdell
Department of Pharmacology, University College London, U K
J Neurochem 68:1812-9. 1997....
Pharmacological properties of alpha 9 alpha 10 nicotinic acetylcholine receptors revealed by heterologous expression of subunit chimerasElizabeth R Baker
Department of Pharmacology, University College London, Gower Street, London, United Kingdom
Mol Pharmacol 65:453-60. 2004..Results have also been compared with radioligand binding data conducted with a previously described alpha7/5HT3A (alpha7chi) subunit chimera...
Incorporation of the beta3 subunit has a dominant-negative effect on the function of recombinant central-type neuronal nicotinic receptorsSteven Broadbent
Department of Pharmacology, University College London, Gower St, London, WC1E 6BT, UK
Mol Pharmacol 70:1350-7. 2006..This raises the possibility of a novel regulatory role for the beta3 subunit on neuronal nicotinic signaling in the central nervous system...
Host-cell specific effects of the nicotinic acetylcholine receptor chaperone RIC-3 revealed by a comparison of human and Drosophila RIC-3 homologuesStuart J Lansdell
Department of Pharmacology, University College London, London, UK
J Neurochem 105:1573-81. 2008..In addition, studies conducted in different expression systems suggest that additional host cell factors may modulate the chaperone activity of RIC-3...
Nicotinic acetylcholine receptor transmembrane mutations convert ivermectin from a positive to a negative allosteric modulatorToby Collins
Department of Neuroscience, Physiology and Pharmacology, University College London, London, United Kingdom
Mol Pharmacol 78:198-204. 2010..We conclude that transmembrane mutations in alpha7 nAChRs are able to convert ivermectin from a positive to a negative allosteric modulator...
Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane siteGareth T Young
Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London WC1E 6BT, United Kingdom
Proc Natl Acad Sci U S A 105:14686-91. 2008..Our findings suggest that this is a conserved modulatory allosteric site within neurotransmitter-gated ion channels...
RIC-3 enhances functional expression of multiple nicotinic acetylcholine receptor subtypes in mammalian cellsStuart J Lansdell
Department of Pharmacology, University College London, Gower St, London, WC1E 6BT United Kingdom
Mol Pharmacol 68:1431-8. 2005..We conclude that RIC-3 is an nAChR-associated protein that can enhance functional expression of multiple nAChR subtypes in transfected mammalian cells...
Molecular characterisation of nicotinic acetylcholine receptor subunits from the cat flea, Ctenocephalides felis (Siphonaptera: Pulicidae)Chris Bass
Department of Biological and Ecological Chemistry, Rothamsted Research, Harpenden, AL5 2JQ, UK
Insect Biochem Mol Biol 36:86-96. 2006....
Rat nicotinic ACh receptor alpha7 and beta2 subunits co-assemble to form functional heteromeric nicotinic receptor channelsSerguei S Khiroug
Laboratory of Signal Transduction, National Institute of Environmental Health Sciences, National Institutes of Health, PO Box 12233, Research Triangle Park, NC 27709, USA
J Physiol 540:425-34. 2002..This co-assembly may help to explain nAChR channel diversity in rat hippocampal interneurons, and perhaps in other areas of the nervous system...
Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165Christopher G V Sharples
Department of Biology and Biochemistry, University of Bath, Bath BA2 7AY, UK
J Med Chem 45:3235-45. 2002..This rational series of compounds based on UB-165 presents a systematic approach to defining subtype specific pharmacophores...
Inhibition of the alpha9alpha10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-D-aspartate receptorsPaola V Plazas
Instituto de Investigaciones en Ingenieria Genetica y Biologia Molecular, Consejo Nacional de Investigaciones Cientificas y Tecnicas, Argentina
Eur J Pharmacol 566:11-9. 2007....
Effects of quinine, quinidine, and chloroquine on alpha9alpha10 nicotinic cholinergic receptorsJimena A Ballestero
, CONICET-UBA, Vuelta de Obligado 2490, 1428 Buenos Aires, Argentina
Mol Pharmacol 68:822-9. 2005....
Pharmacological profiles of recombinant and native insect nicotinic acetylcholine receptorsMotohiro Tomizawa
Environmental Chemistry and Toxicology Laboratory, Department of Environmental Science, Policy and Management, University of California, Berkeley, 94720 3112, USA
Insect Biochem Mol Biol 35:1347-55. 2005..These findings are consistent with the agonist binding site being located at the nAChR subunit interface and indicate that both alpha and beta subunits influence the pharmacological properties of insect nAChRs...
A nicotinic acetylcholine receptor mutation conferring target-site resistance to imidacloprid in Nilaparvata lugens (brown planthopper)Zewen Liu
Key Laboratory of Monitoring and Management of Plant Diseases and Insects, Ministry of Agriculture, Nanjing Agricultural University, Nanjing 210095, China
Proc Natl Acad Sci U S A 102:8420-5. 2005..This study provides direct evidence for the occurrence of target-site resistance to a neonicotinoid insecticide...
Stable expression and characterisation of a human alpha 7 nicotinic subunit chimera: a tool for functional high-throughput screeningPeter J Craig
Eli Lilly and Company Ltd, Lilly Research Centre, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK
Eur J Pharmacol 502:31-40. 2004..Use of this chimera in high-throughput screening may enable the identification of novel pharmacological agents that will help to define further the role of alpha7 nicotinic receptors in physiology and disease...
