(Q34139176)

31 July 2017

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title

Allosteric binding sites on cell-surface receptors: novel targets for drug discovery (English)

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31 July 2017

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Arthur Christopoulos

1

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31 July 2017

1 March 2002

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Nature Reviews Drug Discovery

31 July 2017

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31 July 2017

1

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31 July 2017

3

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31 July 2017

198-210

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https://scigraph.springernature.com/pub.10.1038/nrd746

31 July 2017

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Drug discovery: a historical perspective

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Inverse, protean, and ligand-selective agonism: matters of receptor conformation

31 March 2020

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Conformational substates in proteins

31 March 2020

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The Energy Landscapes and Motions of Proteins

31 March 2020

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Proteins--paradigms of complex systems

31 March 2020

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

31 March 2020

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Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation.

31 March 2020

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G protein-coupled receptor allosterism and complexing

31 March 2020

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An allosteric model for benzodiazepine receptor function

31 March 2020

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Interactions of agonists with an allosteric antagonist at muscarinic acetylcholine M2 receptors

31 March 2020

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Allosteric regulation of muscarinic receptors.

31 March 2020

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Functional domains of GABAA receptors.

31 March 2020

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Allosteric receptors after 30 years

31 March 2020

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From GABAA receptor diversity emerges a unified vision of GABAergic inhibition.

31 March 2020

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Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes.

31 March 2020

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Benzodiazepines on trial: a research strategy for their rehabilitation

31 March 2020

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GABA(A) receptor subtypes: dissecting their pharmacological functions

31 March 2020

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Heterodimerization of G-protein-coupled receptors: pharmacology, signaling and trafficking

31 March 2020

1 reference

Site-directed mutagenesis reveals two epitopes involved in the subtype selectivity of the allosteric interactions of gallamine at muscarinic acetylcholine receptors

31 March 2020

1 reference

Interactions of alcuronium, TMB-8, and other allosteric ligands with muscarinic acetylcholine receptors: studies with chimeric receptors.

31 March 2020

1 reference

Allosteric site on muscarinic acetylcholine receptors: a single amino acid in transmembrane region 7 is critical to the subtype selectivities of caracurine V derivatives and alkane-bisammonium ligands

31 March 2020

1 reference

The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate recepto

31 March 2020

1 reference

Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site

31 March 2020

1 reference

Allosteric interactions at muscarinic cholinoceptors

31 March 2020

1 reference

Characterization of the subtype selectivity of the allosteric modulator heptane-1,7-bis-(dimethyl-3'-phthalimidopropyl) ammonium bromide (C7/3-phth) at cloned muscarinic acetylcholine receptors

31 March 2020

1 reference

Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.

31 March 2020

1 reference

Allosteric modulation of A2A adenosine receptors by amiloride analogues and sodium ions

31 March 2020

1 reference

Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501

31 March 2020

1 reference

BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity

31 March 2020

1 reference

Cooperative multi-modal sensing and therapeutic implications of the extracellular Ca(2+) sensing receptor

31 March 2020

1 reference

Allosteric enhancer PD 81,723 acts by novel mechanism to potentiate cardiac actions of adenosine

31 March 2020

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Use of a spreadsheet to quantitate the equilibrium binding of an allosteric modulator.

31 March 2020

1 reference

Unique allosteric regulation of 5-hydroxytryptamine receptor-mediated signal transduction by oleamide

31 March 2020

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Allosteric regulation by oleamide of the binding properties of 5-hydroxytryptamine7 receptors

31 March 2020

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Application of an allosteric ternary complex model to the technique of pharmacological resultant analysis.

31 March 2020

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Divergent modes of action among cationic allosteric modulators of muscarinic M2 receptors

31 March 2020

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Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation

31 March 2020

1 reference

Teleonomic mechanisms in cellular metabolism, growth, and differentiation

31 March 2020

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Allosteric proteins and cellular control systems

31 March 2020

1 reference

ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL

31 March 2020

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Interaction at End-Plate Receptors between Different Choline Derivatives

31 March 2020

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A study of the desensitization produced by acetylcholine at the motor end-plate

31 March 2020

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On the application of "a plausible model" of allosteric proteins to the receptor for acetylcholine

31 March 2020

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Inhibition of Lysosomal Plasminogen Activator Activity in Experimental Shock

31 March 2020

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The two-state model of receptor activation

31 March 2020

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31 March 2020

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Inhibition of the actions of carbachol and DFP on guinea pig isolated atria by alkane-bis-ammonium compounds

31 March 2020

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The inhibitory effect of gallamine on muscarinic receptors

31 March 2020

1 reference

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

31 March 2020

1 reference

Human eosinophil major basic protein is an endogenous allosteric antagonist at the inhibitory muscarinic M2 receptor

31 March 2020

1 reference

The pharmacology of amino-acid responses in septal neurons.

31 March 2020

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From ion currents to genomic analysis: recent advances in GABAA receptor research.

31 March 2020

1 reference

General anaesthetic action at transmitter-gated inhibitory amino acid receptors

31 March 2020

1 reference

Neuroactive steroids: potential therapeutic use in neurological and psychiatric disorders

31 March 2020

1 reference

γ-Aminobutyric acid regulation of the benzodiazepine receptor: biochemical evidence for pharmacologically different effects of benzodiazepines and propyl β-carboline-3-carboxylate

31 March 2020

1 reference

Interaction of Convulsive Ligands with Benzodiazepine Receptors

31 March 2020

1 reference

Modulation of muscle nicotinic acetylcholine receptors by the glucocorticoid hydrocortisone. Possible allosteric mechanism of channel blockade

31 March 2020

1 reference

The TiPS lecture. The nicotinic acetylcholine receptor: an allosteric protein prototype of ligand-gated ion channels

31 March 2020

1 reference

Cembranoid and long-chain alkanol sites on the nicotinic acetylcholine receptor and their allosteric interaction.

31 March 2020

1 reference

Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor.

31 March 2020

1 reference

Subunit- and site-specific pharmacology of the NMDA receptor channel

31 March 2020

1 reference

D-serine is an endogenous ligand for the glycine site of the N-methyl-D-aspartate receptor

31 March 2020

1 reference

The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential

31 March 2020

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Allosteric interactions and modulator requirement for NMDA receptor function

31 March 2020

1 reference

Polyamines modulate [3H]L-689,560 binding to the glycine site of the NMDA receptor from rat brain.

31 March 2020

1 reference

The allosteric enhancer, PD 81,723, stabilizes human A1 adenosine receptor coupling to G proteins

31 March 2020

1 reference

Differential effects of the allosteric enhancer (2-amino-4,5-dimethyl-trienyl)[3-trifluoromethyl) phenyl]methanone (PD81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor

31 March 2020

1 reference

Allosteric interactions between the antagonist prazosin and amiloride analogs at the human alpha(1A)-adrenergic receptor.

31 March 2020

1 reference

Agonist binding and function at the human alpha(2A)-adrenoceptor: allosteric modulation by amilorides.

31 March 2020

1 reference

Dual interaction of agmatine with the rat alpha(2D)-adrenoceptor: competitive antagonism and allosteric activation

31 March 2020

1 reference

Allosteric modulation of beta2-adrenergic receptor by Zn(2+).

31 March 2020

1 reference

L-amino acid sensing by the extracellular Ca2+-sensing receptor

31 March 2020

1 reference

Human interferon-inducible 10-kDa protein and human interferon-inducible T cell alpha chemoattractant are allotopic ligands for human CXCR3: differential binding to receptor states.

31 March 2020

1 reference

Anti-HIV agent trichosanthin enhances the capabilities of chemokines to stimulate chemotaxis and G protein activation, and this is mediated through interaction of trichosanthin and chemokine receptors

31 March 2020

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A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry.

31 March 2020

1 reference

Zinc allosterically modulates antagonist binding to cloned D1 and D2 dopamine receptors.

31 March 2020

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Allosteric inhibition of endothelin ETA receptors by 3, 5-dibromosalicylic acid.

31 March 2020

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Aspirin and sodium salicylate inhibit endothelin ETA receptors by an allosteric type of mechanism

31 March 2020

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Novel allosteric antagonists shed light on mglu(5) receptors and CNS disorders

31 March 2020

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Complex allosteric interaction of heparin with neurokinin-1 receptors

31 March 2020

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Antagonism of adenosine 5'-triphosphate-induced relaxation by 2-2'-pyridylisatogen in the taenia of guinea-pig caecum

31 March 2020

1 reference

Potentiation by 2,2'-pyridylisatogen tosylate of ATP-responses at a recombinant P2Y1 purinoceptor

31 March 2020

1 reference

A new peptide, 5-HT-moduline, isolated and purified from mammalian brain specifically interacts with 5-HT1B/1D receptors

31 March 2020

1 reference

Molecular, cellular and physiological characteristics of 5-HT-moduline, a novel endogenous modulator of 5-HT1B receptor subtype.

31 March 2020

1 reference

31 March 2020

Identifiers

DOI

10.1038/NRD746

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31 July 2017

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PubMed ID

12120504