(Q24672483)

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Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors

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Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors (English)

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David Colquhoun

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D Colquhoun

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D Colquhoun

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publication date

November 1998

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British Journal of Pharmacology

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125

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924-47

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5

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Binding sites contribute unequally to the gating of mouse nicotinic alpha D200N acetylcholine receptors

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Identification of amino acid residues of the NR2A subunit that control glutamate potency in recombinant NR1/NR2A NMDA receptors

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Some quantitative uses of drug antagonists

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Determination of NMDA NR1 subunit copy number in recombinant NMDA receptors

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Cellular signaling by an agonist-activated receptor/Gs alpha fusion protein

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How receptors talk to trimeric G proteins

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Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins

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Agonist occupation of an alpha2A-adrenoreceptor-Gi1alpha fusion protein results in activation of both receptor-linked and endogenous Gi proteins. Comparisons of their contributions to GTPase activity and signal transduction and analysis of receptor-

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A single residue in the M2-M3 loop is a major determinant of coupling between binding and gating in neuronal nicotinic receptors.

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Allosteric proteins: from regulatory enzymes to receptors--personal recollections.

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Activation kinetics of recombinant mouse nicotinic acetylcholine receptors: mutations of alpha-subunit tyrosine 190 affect both binding and gating

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Identification of tryptophan 55 as the primary site of [3H]nicotine photoincorporation in the gamma-subunit of the Torpedo nicotinic acetylcholine receptor

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The G-protein nanomachine

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The elusive nature of intrinsic efficacy.

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Molecular pharmacology. The binding issue.

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Action of brief pulses of glutamate on AMPA/kainate receptors in patches from different neurones of rat hippocampal slices.

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Fluctuations in the microsecond time range of the current through single acetylcholine receptor ion channels

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Fast events in single-channel currents activated by acetylcholine and its analogues at the frog muscle end-plate

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From muscle endplate to brain synapses: a short history of synapses and agonist-activated ion channels

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Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins

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Interaction at End-Plate Receptors between Different Choline Derivatives

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Cooperative Interactions of Hemoglobin

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Mechanisms of activation of muscle nicotinic acetylcholine receptors and the time course of endplate currents.

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A molecular scheme for the reaction between acetylcholine and nicotinic channels

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Conductances of single ion channels opened by nicotinic agonists are indistinguishable

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Fluorescent labeling of purified beta 2 adrenergic receptor. Evidence for ligand-specific conformational changes

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Activation of N-methyl-D-aspartate receptors by L-glutamate in cells dissociated from adult rat hippocampus.

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Structure‐activity relationships for transmembrane signaling: the receptor's turn

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Currents through single glutamate receptor channels in outside-out patches from rat cerebellar granule cells

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Muscarinic receptor subtypes

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Location of a delta-subunit region determining ion transport through the acetylcholine receptor channel

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Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance

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Single channel currents in the nicotinic acetylcholine receptor: a direct demonstration of allosteric transitions

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Finding affinity constants for agonists by the irreversible antagonists method

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Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins.

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Agonist-specific receptor conformations

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Promiscuity, pre-coupling and instability

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Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins

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Properties of human glycine receptors containing the hyperekplexia mutation alpha1(K276E), expressed in Xenopus oocytes.

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Cuddling up to channel activation

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ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL

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Single cyclic nucleotide-gated channels locked in different ligand-bound states.

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1 reference

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1 reference

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1 reference

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1 reference

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1 reference

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based on heuristic

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1 reference

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based on heuristic

inferred from DOI database lookup

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1 reference

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based on heuristic

inferred from DOI database lookup

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1 reference

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10.1038/SJ.BJP.0702164

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Consolidated OpenCitations Corpus – April 2017

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Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

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Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

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Consolidated OpenCitations Corpus – April 2017

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