Stoichiometry of a ligand-gated ion channel determined by fluorescence energy transfer.
- Authors
- Farrar, S J; Whiting, P J; Bonnert, T P; McKernan, R M
- Year
- 1999
- Journal
- The Journal of biological chemistry
- PMID
- 10187791
- DOI
- 10.1074/jbc.274.15.10100
We have developed a method to determine the stoichiometry of subunits within an oligomeric cell surface receptor using fluorescently tagged antibodies to the individual subunits and measuring energy transfer between them. Anti-c-Myc monoclonal antibody (mAb 9-E10) derivatized with a fluorophore (europium cryptate, EuK) was used to individually label c-Myc-tagged alpha1-, beta2-, or gamma2-subunits of the hetero-oligomeric gamma-aminobutyric acid (GABAA) receptor in intact cells. The maximal fluorescent signal derived from the alpha1(c-Myc)beta2gamma2 and the alpha1beta2(c-Myc)gamma2 receptors was twice that obtained with alpha1beta2gamma2(c-Myc), suggesting that there are 2x alpha-, 2x beta-, and 1x gamma-subunits in a receptor monomer. This observation was extended using fluorescence energy transfer. Receptors were half-maximally saturated with EuK-anti-c-Myc mAb, and the remaining alpha1(c-Myc) subunits were labeled with excess anti-c-Myc mAb derivatized with the fluorescence energy acceptor, XL665. On exposure to laser light, energy transfer from EuK to XL665 occurred with alpha1(c-Myc)beta2gamma2 and alpha1beta2(c-Myc)gamma2, but no significant energy transfer was observed with alpha1beta2gamma2(c-Myc) receptors, indicating the absence of a second gamma-subunit in a receptor monomer. We confirm that the GABAA receptor subtype, alpha1beta2gamma2, is composed of two copies each of the alpha- and beta-subunits and one copy of the gamma-subunit (i.e. (alpha1)2(beta2)2(gamma2)1) and conclude that this method would have general applicability to other multisubunit cell surface proteins.
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In this knowledge base
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| Benzodiazepines affect channel opening of GABA A receptors induced by either agonist binding site. | Baur R et al. | β | 2005 | β |
| Conformational changes at benzodiazepine binding sites of GABA(A) receptors detected with a novel technique. | Berezhnoy D et al. | β | 2005 | β |
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| Enhancement of benzodiazepine binding sites following chronic treatment with flumazenil. | PericiΔ D et al. | β | 2005 | β |
| Functional and structural analysis of the GABAA receptor alpha 1 subunit during channel gating and alcohol modulation. | Jung S et al. | β | 2005 | β |
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| Proton modulation of recombinant GABA(A) receptors: influence of GABA concentration and the beta subunit TM2-TM3 domain. | Wilkins ME et al. | β | 2005 | β |
| Variations on an inhibitory theme: phasic and tonic activation of GABA(A) receptors. | Farrant M et al. | β | 2005 | β |
| 3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors. | Szekeres HJ et al. | β | 2004 | β |
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| An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties. | Chambers MS et al. | β | 2004 | β |
| Atomic force microscopy and drug discovery. | Edwardson JM et al. | β | 2004 | β |
| Brain regional heterogeneity of pH effects on GABA(A) receptor-associated [35s]TBPS binding. | Uusi-Oukari M et al. | β | 2004 | β |
| Chronic exposure of cells expressing recombinant GABAA receptors to benzodiazepine antagonist flumazenil enhances the maximum number of benzodiazepine binding sites. | PericiΔ D et al. | β | 2004 | β |
| Compounds exhibiting selective efficacy for different beta subunits of human recombinant gamma-aminobutyric acid A receptors. | Smith AJ et al. | β | 2004 | β |
| Functional mapping of GABA A receptor subtypes in the amygdala. | Marowsky A et al. | β | 2004 | β |
| GABAA receptor structure-function studies: a reexamination in light of new acetylcholine receptor structures. | Akabas MH | β | 2004 | β |
| Gating allosterism at a single class of etomidate sites on alpha1beta2gamma2L GABA A receptors accounts for both direct activation and agonist modulation. | RΓΌsch D et al. | β | 2004 | β |
| Genetic manipulations of GABAA receptor in mice make inhibition exciting. | Vicini S et al. | β | 2004 | β |
| Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. | Derry JM et al. | β | 2004 | β |
| Mutation of glutamate 155 of the GABAA receptor beta2 subunit produces a spontaneously open channel: a trigger for channel activation. | Newell JG et al. | β | 2004 | β |
| On the benzodiazepine binding pocket in GABAA receptors. | Berezhnoy D et al. | β | 2004 | β |
| Positioning of the alpha-subunit isoforms confers a functional signature to gamma-aminobutyric acid type A receptors. | Minier F et al. | β | 2004 | β |
| Regulation of GABAA receptor trafficking, channel activity, and functional plasticity of inhibitory synapses. | LΓΌscher B et al. | β | 2004 | β |
| Salicylidene salicylhydrazide, a selective inhibitor of beta 1-containing GABAA receptors. | Thompson SA et al. | β | 2004 | β |
| Chronic ethanol consumption enhances internalization of alpha1 subunit-containing GABAA receptors in cerebral cortex. | Kumar S et al. | β | 2003 | β |
| Constitutive GABAA receptor endocytosis is dynamin-mediated and dependent on a dileucine AP2 adaptin-binding motif within the beta 2 subunit of the receptor. | Herring D et al. | β | 2003 | β |
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| Formation and plasticity of GABAergic synapses: physiological mechanisms and pathophysiological implications. | Fritschy JM et al. | β | 2003 | β |
| GABA(A) receptor composition is determined by distinct assembly signals within alpha and beta subunits. | Bollan K et al. | β | 2003 | β |
| GABARAP: lessons for synaptogenesis. | Coyle JE et al. | β | 2003 | β |
| Identification of an amino acid sequence within GABA(A) receptor beta3 subunits that is important for receptor assembly. | Ehya N et al. | β | 2003 | β |
| Individual properties of the two functional agonist sites in GABA(A) receptors. | Baumann SW et al. | β | 2003 | β |
| Intact synaptic GABAergic inhibition and altered neurosteroid modulation of thalamic relay neurons in mice lacking delta subunit. | Porcello DM et al. | β | 2003 | β |
| Major differences in inhibitory synaptic transmission onto two neocortical interneuron subclasses. | Bacci A et al. | β | 2003 | β |
| On high- and low-affinity agonist sites in GABAA receptors. | Baur R et al. | β | 2003 | β |
| Zinc-mediated inhibition of GABA(A) receptors: discrete binding sites underlie subtype specificity. | Hosie AM et al. | β | 2003 | β |
| Assembly and cell surface expression of homomeric and heteromeric 5-HT3 receptors: the role of oligomerization and chaperone proteins. | Boyd GW et al. | β | 2002 | β |
| Direct visualization of ligand-protein interactions using atomic force microscopy. | Neish CS et al. | β | 2002 | β |
| Electrophysiological actions of gamma-aminobutyric acid and clomethiazole on recombinant GABA(A) receptors. | Nelson RM et al. | β | 2002 | β |
| Forced subunit assembly in alpha1beta2gamma2 GABAA receptors. Insight into the absolute arrangement. | Baumann SW et al. | β | 2002 | β |
| Functional consequences of the loss of high affinity agonist binding to gamma-aminobutyric acid type A receptors. Implications for receptor desensitization. | Newell JG et al. | β | 2002 | β |
| GABA(A) receptor beta 2 Tyr97 and Leu99 line the GABA-binding site. Insights into mechanisms of agonist and antagonist actions. | Boileau AJ et al. | β | 2002 | β |
| GABAergic innervation organizes synaptic and extrasynaptic GABAA receptor clustering in cultured hippocampal neurons. | Christie SB et al. | β | 2002 | β |
| Glycine and GABA(A) receptor subunits on Renshaw cells: relationship with presynaptic neurotransmitters and postsynaptic gephyrin clusters. | Geiman EJ et al. | β | 2002 | β |
| Homologous sites of GABA(A) receptor alpha(1), beta(3) and gamma(2) subunits are important for assembly. | Sarto I et al. | β | 2002 | β |
| Ivermectin and nodulisporic acid receptors in Drosophila melanogaster contain both gamma-aminobutyric acid-gated Rdl and glutamate-gated GluCl alpha chloride channel subunits. | Ludmerer SW et al. | β | 2002 | β |
| Neonatal development of the rat visual cortex: synaptic function of GABAA receptor alpha subunits. | Bosman LW et al. | β | 2002 | β |
| Overexpression of the GABA(A) receptor epsilon subunit results in insensitivity to anaesthetics. | Thompson SA et al. | β | 2002 | β |
| Principles and biophysical applications of lanthanide-based probes. | Selvin PR | β | 2002 | β |
| Structure of GABARAP in two conformations: implications for GABA(A) receptor localization and tubulin binding. | Coyle JE et al. | β | 2002 | β |
| The relative amount of cRNA coding for gamma2 subunits affects stimulation by benzodiazepines in GABA(A) receptors expressed in Xenopus oocytes. | Boileau AJ et al. | β | 2002 | β |
| Time resolved amplification of cryptate emission: a versatile technology to trace biomolecular interactions. | Bazin H et al. | β | 2002 | β |
| Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptors. | Thompson SA et al. | β | 2002 | β |
| Tryptophan scanning mutagenesis in TM4 of the GABA(A) receptor alpha1 subunit: implications for modulation by inhaled anesthetics and ion channel structure. | Jenkins A et al. | β | 2002 | β |
| alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. | Adkins CE et al. | β | 2001 | β |
| Constructing inhibitory synapses. | Moss SJ et al. | β | 2001 | β |
| Detection and binding properties of GABA(A) receptor assembly intermediates. | Klausberger T et al. | β | 2001 | β |
| Evidence for distinct conformations of the two alpha 1 subunits in diazepam-bound GABA(A) receptors. | Williams DB et al. | β | 2001 | β |
| Evidence for the formation of functionally distinct alphabetagammaepsilon GABA(A) receptors. | Davies PA et al. | β | 2001 | β |
| GABA(A) receptor epsilon-subunit may confer benzodiazepine insensitivity to the caudal aspect of the nucleus tractus solitarii of the rat. | Kasparov S et al. | β | 2001 | β |
| Homogeneous time resolved fluorescence resonance energy transfer using rare earth cryptates as a tool for probing molecular interactions in biology. | Bazin H et al. | β | 2001 | β |
| Molecular determinants of desensitization and assembly of the chimeric GABA(A) receptor subunits (alpha1/gamma2) and (gamma2/alpha1) in combinations with beta2 and gamma2. | Elster L et al. | β | 2001 | β |
| Monitoring receptor oligomerization using time-resolved fluorescence resonance energy transfer and bioluminescence resonance energy transfer. The human delta -opioid receptor displays constitutive oligomerization at the cell surface, which is not regulated by receptor occupancy. | McVey M et al. | β | 2001 | β |
| Prevalence between different alpha subunits performing the benzodiazepine binding sites in native heterologous GABA(A) receptors containing the alpha2 subunit. | del RΓo JC et al. | β | 2001 | β |
| Protein mobility and GABA-induced conformational changes in GABA(A) receptor pore-lining M2 segment. | Horenstein J et al. | β | 2001 | β |
| The non-peptidyl fungal metabolite L-783,281 activates TRK neurotrophin receptors. | Wilkie N et al. | β | 2001 | β |
| Benzodiazepines induce a conformational change in the region of the gamma-aminobutyric acid type A receptor alpha(1)-subunit M3 membrane-spanning segment. | Williams DB et al. | β | 2000 | β |
| Development of a time-resolved fluorometric detection system using diffusion-enhanced energy transfer | Koresawa M et al. | β | 2000 | β |
| Fluorescence properties of pyrylretinol. | Das J et al. | β | 2000 | β |
| GABA potentiation: a logical pharmacological approach for the treatment of acute ischaemic stroke. | Green AR et al. | β | 2000 | β |
| Influence of subunit configuration on the interaction of picrotoxin-site ligands with recombinant GABA(A) receptors. | Bell-Horner CL et al. | β | 2000 | β |
| N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. | Collins I et al. | β | 2000 | β |
| The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations. | Krasowski MD et al. | β | 2000 | β |
| Tryptophan scanning mutagenesis in TM2 of the GABA(A) receptor alpha subunit: effects on channel gating and regulation by ethanol. | Ueno S et al. | β | 2000 | β |
| Two conserved arginines in the extracellular N-terminal domain of the GABA(A) receptor alpha(5) subunit are crucial for receptor function. | Hartvig L et al. | β | 2000 | β |
| Tyrosine 62 of the gamma-aminobutyric acid type A receptor beta 2 subunit is an important determinant of high affinity agonist binding. | Newell JG et al. | β | 2000 | β |
| Gamma-aminobutyric acid increases the water accessibility of M3 membrane-spanning segment residues in gamma-aminobutyric acid type A receptors. | Williams DB et al. | β | 1999 | β |