Allosteric modulation of G-protein coupled receptors

Crystal Structure of Rhodopsin: A G Protein-Coupled Receptor

2000 • 5,539 citations

Seven-transmembrane receptors

2002 • 2,571 citations

A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

1993 • 1,213 citations

PDZ Domains and the Organization of Supramolecular Complexes

2001 • 1,203 citations

Uncovering Molecular Mechanisms Involved in Activation of G Protein-Coupled Receptors

2000 • 1,199 citations

Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor

2000 • 1,197 citations

Neurobiology of Zinc and Zinc-Containing Neurons

1989 • 1,075 citations

G Protein-Coupled Receptor Allosterism and Complexing

2002 • 910 citations

A New Benzodiazepine Pharmacology

2002 • 706 citations

Organization of the G Protein-coupled Receptors Rhodopsin and Opsin in Native Membranes

2003 • 591 citations

Dimerization: An Emerging Concept for G Protein–Coupled Receptor Ontogeny and Function

2002 • 580 citations

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

1989 • 519 citations

The two-state model of receptor activation

1995 • 492 citations

<scp>l</scp> -Amino acid sensing by the extracellular Ca ²⁺ -sensing receptor

2000 • 484 citations

Homer: a link between neural activity and glutamate receptor function

2000 • 405 citations

Structural views of the ligand-binding cores of a metabotropic glutamate receptor complexed with an antagonist and both glutamate and Gd ³⁺

2002 • 337 citations

Uncovering Molecular Mechanisms Involved in Activation of G Protein-Coupled Receptors

2000 • 329 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

Ligand-selective receptor conformations revisited: the promise and the problem

2003 • 319 citations

An aspartate conserved among G-protein receptors confers allosteric regulation of alpha 2-adrenergic receptors by sodium.

1990 • 266 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

THE INHIBITORY EFFECT OF GALLAMINE ON MUSCARINIC RECEPTORS

1976 • 249 citations

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.

2001 • 242 citations

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

2001 • 236 citations

Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment

2003 • 235 citations

Positive Cooperativity of Acetylcholine and Other Agonists with Allosteric Ligands on Muscarinic Acetylcholine Receptors

1997 • 222 citations

Positive Allosteric Modulation of Native and Recombinant γ-Aminobutyric Acid_B Receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its Aldehyde Analog CGP13501

2001 • 219 citations

A Small Molecule Antagonist of Chemokine Receptors CCR1 and CCR3

2000 • 218 citations

Structural Basis for a Ca ²⁺ -Sensing Function of the Metabotropic Glutamate Receptors

1998 • 216 citations

A Family of Highly Selective Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5

2003 • 209 citations

Regulator of G protein signaling proteins: novel multifunctional drug targets.

2001 • 205 citations

(−)-PHCCC, a positive allosteric modulator of mGluR4: characterization, mechanism of action, and neuroprotection

2003 • 199 citations

Lessons from constitutively active mutants of G protein-coupled receptors

2002 • 192 citations

Constitutive activation of a single effector pathway: evidence for multiple activation states of a G protein-coupled receptor.

1996 • 188 citations

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

2000 • 188 citations

Discovery of an Ectopic Activation Site on the M₁Muscarinic Receptor

2002 • 187 citations

Pivotal role for aspartate-80 in the regulation of dopamine D2 receptor affinity for drugs and inhibition of adenylyl cyclase.

1991 • 185 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

Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB‐1893 and MPEP

2003 • 174 citations

BAY36-7620: A Potent Non-Competitive mGlu1 Receptor Antagonist with Inverse Agonist Activity.

2001 • 166 citations

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

2003 • 159 citations

Allosteric modulation of muscarinic acetylcholine receptors

1995 • 155 citations

Mutational Analysis and Molecular Modeling of the Binding Pocket of the Metabotropic Glutamate 5 Receptor Negative Modulator 2-Methyl-6-(phenylethynyl)-pyridine

2003 • 145 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

The Neurokinin A Receptor Activates Calcium and cAMP Responses through Distinct Conformational States

2001 • 129 citations

Modeling and Mutagenesis of the Binding Site of Calhex 231, a Novel Negative Allosteric Modulator of the Extracellular Ca2+-sensing Receptor

2003 • 128 citations

G _sα -selective G protein antagonists

1998 • 126 citations

G protein antagonists

1999 • 125 citations

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

1997 • 123 citations

Allosteric activation of the Ca2+ receptor expressed in Xenopus laevis oocytes by NPS 467 or NPS 568.

1998 • 123 citations

Subtype-Selective Positive Cooperative Interactions between Brucine Analogues and Acetylcholine at Muscarinic Receptors: Radioligand Binding Studies

1998 • 118 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

Domains determining ligand specificity for Ca2+ receptors.

1999 • 115 citations

Identification of Allosteric Peptide Agonists of CXCR4

2003 • 112 citations

Allosteric Interactions of Staurosporine and Other Indolocarbazoles withN-[methyl-³H]Scopolamine and Acetylcholine at Muscarinic Receptor Subtypes: Identification of a Second Allosteric Site

2000 • 111 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

Conversion of agonist site to metal-ion chelator site in the β ₂ -adrenergic receptor

1999 • 108 citations

Three Adjacent Serines in the Extracellular Domains of the CaR Are Required for l-Amino Acid-mediated Potentiation of Receptor Function

2002 • 105 citations

Metal Ion-mediated Agonism and Agonist Enhancement in Melanocortin MC1 and MC4 Receptors

2002 • 102 citations

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

2000 • 101 citations

Allosteric Modulation of β₂-Adrenergic Receptor by Zn²⁺

2002 • 95 citations

Subtype-selective positive cooperative interactions between brucine analogs and acetylcholine at muscarinic receptors: functional studies.

1999 • 93 citations

Site-Directed Mutagenesis Reveals Two Epitopes Involved in the Subtype Selectivity of the Allosteric Interactions of Gallamine at Muscarinic Acetylcholine Receptors

1999 • 93 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

Analogs of WIN 62,577 Define a Second Allosteric Site on Muscarinic Receptors

2002 • 89 citations

The NMDA Receptor Complex: A Promising Target for Novel Antiepileptic Strategies

2001 • 89 citations

Identification of a Ligand-dependent Switch within a Muscarinic Receptor

1998 • 88 citations

Identification of an Allosteric Binding Site for Zn2+on the β2 Adrenergic Receptor

2002 • 87 citations

5-hydroxytryptamine-moduline, a new endogenous cerebral peptide, controls the serotonergic activity via its specific interaction with 5-hydroxytryptamine1B/1D receptors.

1996 • 85 citations

Two allosteric modulators interact at a common site on cardiac muscarinic receptors.

1992 • 82 citations

SCH-202676: An Allosteric Modulator of Both Agonist and Antagonist Binding to G Protein-Coupled Receptors

2001 • 81 citations

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

2003 • 80 citations

Zinc Allosterically Modulates Antagonist Binding to Cloned D₁ and D₂ Dopamine Receptors

1997 • 80 citations

Allosteric Modulation of A₃Adenosine Receptors by a Series of 3-(2-Pyridinyl)isoquinoline Derivatives

2001 • 77 citations

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

1969 • 77 citations

Modeling and Mutational Analysis of a Putative Sodium-Binding Pocket on the Dopamine D₂Receptor

2001 • 74 citations

Constitutively ActiveAlpha-1b Adrenergic Receptor Mutants Display Different Phosphorylation and Internalization Features

1999 • 73 citations

Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors.

1990 • 70 citations

Pivotal Role of an Aspartate Residue in Sodium Sensitivity and Coupling to G Proteins of Neurotensin Receptors

1999 • 68 citations

G-protein-coupled receptors for neurotransmitter amino acids: C-terminal tails, crowded signalosomes

2002 • 66 citations

Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors.

1994 • 60 citations

Selective allosteric enhancement of the binding and actions of acetylcholine at muscarinic receptor subtypes

1997 • 59 citations

Divergent Modes of Action among Cationic Allosteric Modulators of Muscarinic M₂Receptors

1997 • 59 citations

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

2002 • 57 citations

Partial Agonism through a Zinc-Ion Switch Constructed between Transmembrane Domains III and VII in the Tachykinin NK₁Receptor

2000 • 56 citations

Allosteric α1-Adrenoreceptor Antagonism by the Conopeptide ρ-TIA

2003 • 56 citations

Constitutive Activation of the m5 Muscarinic Receptor by a Series of Mutations at the Extracellular End of Transmembrane 6

1997 • 56 citations

Zinc modulates antagonist interactions with D2-like dopamine receptors through distinct molecular mechanisms.

1999 • 55 citations

The binding-site crevice of the D4 dopamine receptor is coupled to three distinct sites of allosteric modulation.

2001 • 51 citations

Use of chimeric muscarinic receptors to investigate epitopes involved in allosteric interactions.

1993 • 51 citations

Regulation of D2 dopamine receptors by amiloride and amiloride analogs.

1996 • 50 citations

Reassessment of the Ca2+ Sensing Property of a Type I Metabotropic Glutamate Receptor by Simultaneous Measurement of Inositol 1,4,5-Trisphosphate and Ca2+ in Single Cells

2001 • 50 citations

Interactions of Alcuronium, TMB-8, and Other Allosteric Ligands with Muscarinic Acetylcholine Receptors: Studies with Chimeric Receptors

2000 • 50 citations

Changes of cooperativity between N-methylscopolamine and allosteric modulators alcuronium and gallamine induced by mutations of external loops of muscarinic M(3) receptors.

2001 • 48 citations

Scanning Mutagenesis Studies of the M 1 Muscarinic Acetylcholine Receptor

2003 • 47 citations

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

2002 • 45 citations

Positive Allosteric Modulator of the Human 5-HT_2CReceptor

2003 • 44 citations

Agonist-independent effect of an allosteric enhancer of the A1 adenosine receptor in CHO cells stably expressing the recombinant human A1 receptor.

1997 • 41 citations

Allosteric Interactions between the Antagonist Prazosin and Amiloride Analogs at the Human α_1A-Adrenergic Receptor

2000 • 40 citations

Natural agonist enhancing bis‐His zinc‐site in transmembrane segment V of the tachykinin NK₃ receptor

1998 • 36 citations

Allosteric Modulation of the Human 5-HT_7AReceptor by Lipidic Amphipathic Compounds

2001 • 31 citations

Agonist Binding and Function at the Human α_2A-Adrenoceptor: Allosteric Modulation by Amilorides

2000 • 30 citations

Patent status of the therapeutically important G-protein-coupled receptors

2001 • 29 citations

The dance of the clams: twists and turns in the family C GPCR homodimer

2002 • 26 citations

A new peptide, 5-HT-moduline, isolated and purified from mammalian brain specifically interacts with 5-HT1B1D receptors

1995 • 22 citations

Scanning Mutagenesis Studies of the M 1 Muscarinic Acetylcholine Receptor

2003 • 14 citations