G-protein-coupled receptor allosterism: the promise and the problem(s)

On the nature of allosteric transitions: A plausible model

1965 • 8,699 citations

Allosteric proteins and cellular control systems

1963 • 2,187 citations

G Protein-Coupled Receptor Allosterism and Complexing

2002 • 910 citations

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

1998 • 880 citations

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

2002 • 640 citations

International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology

2003 • 603 citations

Functionally Different Agonists Induce Distinct Conformations in the G Protein Coupling Domain of the β2Adrenergic Receptor

2001 • 361 citations

Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods.

1988 • 335 citations

CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding.

1999 • 324 citations

Modification of the binding properties of muscarinic receptors by gallamine.

1983 • 321 citations

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 Receptors

2000 • 263 citations

Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors.

1995 • 259 citations

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

2001 • 236 citations

Current Protocols in Pharmacology

2001 • 208 citations

Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation

2000 • 188 citations

N,N′-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and Structurally Related Compounds: Novel Allosteric Enhancers of γ-Aminobutyric Acid_B Receptor Function

2003 • 184 citations

Pharmacological Characterization and Identification of Amino Acids Involved in the Positive Modulation of Metabotropic Glutamate Receptor Subtype 2

2003 • 159 citations

Mutational Analysis and Molecular Modeling of the Allosteric Binding Site of a Novel, Selective, Noncompetitive Antagonist of the Metabotropic Glutamate 1 Receptor

2003 • 134 citations

Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis.

1995 • 130 citations

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

1997 • 123 citations

[³H]R214127: A Novel High-Affinity Radioligand for the mGlu1 Receptor Reveals a Common Binding Site Shared by Multiple Allosteric Antagonists

2003 • 117 citations

Naturally occurring mutations of the extracellular Ca2+-sensing receptor: implications for its structure and function

2003 • 114 citations

Identification of Allosteric Peptide Agonists of CXCR4

2003 • 112 citations

A model for the functioning of family 3 GPCRs

2002 • 110 citations

Activation of muscarinic acetylcholine receptors via their allosteric binding sites.

1996 • 109 citations

ALLOSTERIC INTERACTIONS AT MUSCARINIC CHOLINOCEPTORS

1998 • 106 citations

Thiochrome Enhances Acetylcholine Affinity at Muscarinic M₄Receptors: Receptor Subtype Selectivity via Cooperativity Rather than Affinity

2004 • 105 citations

Allosteric Site on Muscarinic Acetylcholine Receptors: Identification of Two Amino Acids in the Muscarinic M₂Receptor That Account Entirely for the M₂/M₅Subtype Selectivities of Some Structurally Diverse Allosteric Ligands inN-Methylscopolamine-Occupied Receptors

2003 • 91 citations

Mechanisms of steric and cooperative actions of alcuronium on cardiac muscarinic acetylcholine receptors.

1994 • 91 citations

Allosteric modulators of G-protein-coupled receptors

2003 • 81 citations

Identification of Essential Residues Involved in the Allosteric Modulation of the Human A₃Adenosine Receptor

2003 • 80 citations

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

1996 • 77 citations

GPCR Drug Discovery Through the Exploitation of Allosteric Drug Binding Sites

2002 • 60 citations

Identification of a [³H]Ligand for the Common Allosteric Site of Muscarinic Acetylcholine M₂ Receptors

1998 • 58 citations

Application of a Kinetic Model to the Apparently Complex Behavior of Negative and Positive Allosteric Modulators of Muscarinic Acetylcholine Receptors

2004 • 55 citations

Investigation of the Interaction of a Putative Allosteric Modulator,N-(2,3-Diphenyl-1,2,4-thiadiazole-5-(2H)-ylidene) Methanamine Hydrobromide (SCH-202676), with M₁Muscarinic Acetylcholine Receptors

2003 • 47 citations

Allosteric Modulation of Muscarinic Receptor Signaling: Alcuronium-Induced Conversion of Pilocarpine from an Agonist into an Antagonist

2002 • 45 citations

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

1999 • 37 citations

Chapter 12 Allosteric regulation of muscarinic receptors

1996 • 33 citations

Allosteric modulation of G protein-coupled receptors.

2002 • 28 citations

Plasmon-waveguide resonance spectroscopy: a new tool for investigating signal transduction by G-protein coupled receptors

2003 • 8 citations