Seven-transmembrane receptors: crystals clarify

Initial sequencing and analysis of the human genome

2001 • 23,520 citations

The Sequence of the Human Genome

2001 • 13,500 citations

Crystal Structure of Rhodopsin: A G Protein-Coupled Receptor

2000 • 5,539 citations

[19] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors

1995 • 2,811 citations

Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors

2001 • 1,736 citations

G Protein-coupled Receptors

1998 • 1,292 citations

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

2000 • 1,199 citations

The 2.0 Å crystal structure of a heterotrimeric G protein

1996 • 1,118 citations

Sequence Alignment of the G-Protein Coupled Receptor Superfamily

1992 • 847 citations

Substitution of three amino acids switches receptor specificity of Gqα to that of Giα

1993 • 702 citations

An alpha-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors 1 1Edited by R. Huber

1997 • 639 citations

Advances in Determination of a High-Resolution Three-Dimensional Structure of Rhodopsin, a Model of G-Protein-Coupled Receptors (GPCRs)^,

2001 • 598 citations

How receptors talk to trimeric G proteins

1997 • 562 citations

Molecular Biology of Muscarinic Acetylcholine Receptors

1996 • 488 citations

Structural Mimicry in G Protein-Coupled Receptors: Implications of the High-Resolution Structure of Rhodopsin for Structure-Function Analysis of Rhodopsin-Like Receptors

2001 • 442 citations

Activation of rhodopsin: new insights from structural and biochemical studies

2001 • 406 citations

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

2001 • 361 citations

Three-dimensional models of neurotransmitter G-binding protein-coupled receptors.

1991 • 330 citations

Structural Features and Light-Dependent Changes in the Cytoplasmic Interhelical E−F Loop Region of Rhodopsin: A Site-Directed Spin-Labeling Study

1996 • 259 citations

Functional Microdomains in G-protein-coupled Receptors

1998 • 238 citations

Movement of Retinal Along the Visual Transduction Path

2000 • 218 citations

Mutation of a Highly Conserved Aspartic Acid in the β₂Adrenergic Receptor: Constitutive Activation, Structural Instability, and Conformational Rearrangement of Transmembrane Segment 6

1999 • 203 citations

The activation process of the α _1B -adrenergic receptor: Potential role of protonation and hydrophobicity of a highly conserved aspartate

1997 • 196 citations

Similar Structures and Shared Switch Mechanisms of the β2-Adrenoceptor and the Parathyroid Hormone Receptor

1999 • 186 citations

The effect of mutations in the DRY motif on the constitutive activity and structural instability of the histamine H(2) receptor.

2000 • 184 citations

Molecular basis of muscarinic receptor function

1993 • 181 citations

Conformational Changes in Rhodopsin

1999 • 168 citations

Mapping Light-Dependent Structural Changes in the Cytoplasmic Loop Connecting Helixes C and D in Rhodopsin: A Site-Directed Spin Labeling Study

1995 • 160 citations

Mutation of the Fourth Cytoplasmic Loop of Rhodopsin Affects Binding of Transducin and Peptides Derived from the Carboxyl-terminal Sequences of Transducin α and γ Subunits

2000 • 159 citations

Receptor activation: what does the rhodopsin structure tell us?

2001 • 156 citations

Constitutive Activation of Opsin by Mutation of Methionine 257 on Transmembrane Helix 6

1998 • 141 citations

Agonist-induced Conformational Changes at the Cytoplasmic Side of Transmembrane Segment 6 in the β2 Adrenergic Receptor Mapped by Site-selective Fluorescent Labeling

2001 • 140 citations

Role of the intradiscal domain in rhodopsin assembly and function.

1990 • 139 citations

Muscarinic acetylcholine receptors. Peptide sequencing identifies residues involved in antagonist binding and disulfide bond formation.

1990 • 138 citations

Mapping of contact sites in complex formation between transducin and light-activated rhodopsin by covalent crosslinking: Use of a photoactivatable reagent

2001 • 137 citations

The Amino Terminus of the Fourth Cytoplasmic Loop of Rhodopsin Modulates Rhodopsin-Transducin Interaction

2000 • 133 citations

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

1995 • 130 citations

Structure and function in rhodopsin: replacement by alanine of cysteine residues 110 and 187, components of a conserved disulfide bond in rhodopsin, affects the light-activated metarhodopsin II state.

1994 • 126 citations

Site-directed mutagenesis of the rat m1 muscarinic acetylcholine receptor. Role of conserved cysteines in receptor function.

1992 • 126 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

Effects of Guanine, Inosine, and Xanthine Nucleotides on β₂-Adrenergic Receptor/G_sInteractions: Evidence for Multiple Receptor Conformations

1999 • 109 citations

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

1999 • 108 citations

Mapping of contact sites in complex formation between light-activated rhodopsin and transducin by covalent crosslinking: Use of a chemically preactivated reagent

2001 • 101 citations

Insights into ligand pharmacology using receptor–G-protein fusion proteins

2000 • 101 citations

Identification of Gβγ Binding Sites in the Third Intracellular Loop of the M3-muscarinic Receptor and Their Role in Receptor Regulation

2000 • 101 citations

Rhodopsin/transducin interactions. I. Characterization of the binding of the transducin-beta gamma subunit complex to rhodopsin using fluorescence spectroscopy.

1992 • 100 citations

Structural Features and Light-Dependent Changes in the Sequence 306−322 Extending from Helix VII to the Palmitoylation Sites in Rhodopsin: A Site-Directed Spin-Labeling Study^,

1999 • 98 citations

Receptor and Membrane Interaction Sites on Gβ

1996 • 97 citations

Molecular Basis of Receptor/G Protein Coupling Selectivity Studied by Coexpression of Wild Type and Mutant m2 Muscarinic Receptors with Mutant Gα_q Subunits

1997 • 96 citations

Activating and Inactivating Mutations in N- and C-terminal i3 Loop Junctions of Muscarinic Acetylcholine Hm1 Receptors

1995 • 94 citations

The Functional Topography of Transmembrane Domain 3 of the M1 Muscarinic Acetylcholine Receptor, Revealed by Scanning Mutagenesis

1999 • 93 citations

Structure and function in rhodopsin: Rhodopsin mutants with a neutral amino acid at E134 have a partially activated conformation in the dark state

1997 • 89 citations

Identification of a Ligand-dependent Switch within a Muscarinic Receptor

1998 • 88 citations

The Role of the Aspartate-Arginine-Tyrosine Triad in the m1 Muscarinic Receptor: Mutations of Aspartate 122 and Tyrosine 124 Decrease Receptor Expression but Do Not Abolish Signaling

1997 • 85 citations

Transmembrane Domains 4 and 7 of the M1Muscarinic Acetylcholine Receptor Are Critical for Ligand Binding and the Receptor Activation Switch

2001 • 84 citations

The Functional Microdomain in Transmembrane Helices 2 and 7 Regulates Expression, Activation, and Coupling Pathways of the Gonadotropin-releasing Hormone Receptor

1999 • 83 citations

An Activation Switch in the Ligand Binding Pocket of the C5a Receptor

2001 • 77 citations

A Proposed Structure for Transmembrane Segment 7 of G Protein-Coupled Receptors Incorporating an Asn-Pro/Asp-Pro Motif

1998 • 73 citations

Conserved Extracellular Cysteine Pair in the M₃ Muscarinic Acetylcholine Receptor Is Essential for Proper Receptor Cell Surface Localization but Not for G Protein Coupling

1999 • 70 citations

Genetic Analysis of Receptor-Gαq Coupling Selectivity

1997 • 70 citations

The N-terminal Extension of Gαq Is Critical for Constraining the Selectivity of Receptor Coupling

1997 • 70 citations

Light-induced exposure of the cytoplasmic end of transmembrane helix seven in rhodopsin

1998 • 67 citations

Charged amino acids required for signal transduction by the m3 muscarinic acetylcholine receptor.

1993 • 67 citations

Alanine-Scanning Mutagenesis of Transmembrane Domain 6 of the M₁Muscarinic Acetylcholine Receptor Suggests that Tyr381 Plays Key Roles in Receptor Function

1999 • 66 citations

Constitutive Activation of G Protein-Coupled Receptors as a Result of Selective Substitution of a Conserved Leucine Residue in Transmembrane Helix III

2000 • 62 citations

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

2000 • 56 citations

Genetic Mapping of the Human C5a Receptor

2000 • 56 citations

Single-Cysteine Substitution Mutants at Amino Acid Positions 55−75, the Sequence Connecting the Cytoplasmic Ends of Helices I and II in Rhodopsin: Reactivity of the Sulfhydryl Groups and Their Derivatives Identifies a Tertiary Structure that Changes upon Light-Activation^,

1999 • 53 citations

The conformational switch in 7-transmembrane receptors: the muscarinic receptor paradigm

1999 • 50 citations

Phe310 in Transmembrane VI of the α1B-Adrenergic Receptor Is a Key Switch Residue Involved in Activation and Catecholamine Ring Aromatic Bonding

1999 • 47 citations

Evidence for a Tandem Two-site Model of Ligand Binding to Muscarinic Acetylcholine Receptors

2000 • 44 citations

State-Dependent Disulfide Cross-Linking in Rhodopsin

1999 • 42 citations

Alanine scanning mutagenesis of conserved arginine/lysine-arginine/lysine-X-X-arginine/lysine G protein-activating motifs on m1 muscarinic acetylcholine receptors.

1996 • 42 citations

A Network of Conserved Intramolecular Contacts Defines the Off-state of the Transmembrane Switch Mechanism in a Seven-transmembrane Receptor

2000 • 42 citations

Scanning Mutagenesis Identifies Amino Acid Side Chains in Transmembrane Domain 5 of the M₁Muscarinic Receptor that Participate in Binding the Acetyl Methyl Group of Acetylcholine

2000 • 41 citations

Chloroethylclonidine Binds Irreversibly to Exposed Cysteines in the Fifth Membrane-Spanning Domain of the Human α_2A-Adrenergic Receptor

1998 • 33 citations

Roles of the Transducin α-Subunit α4-Helix/α4-β6 Loop in the Receptor and Effector Interactions

1999 • 30 citations

Activation of Guanosine 5′-[γ-³⁵S]thio-triphosphate Binding through M₁Muscarinic Receptors in Transfected Chinese Hamster Ovary Cell Membranes: 1. Mathematical Analysis of Catalytic G Protein Activation

2001 • 19 citations

Activation of Guanosine 5′-[γ-³⁵S]thio-triphosphate Binding through M₁Muscarinic Receptors in Transfected Chinese Hamster Ovary Cell Membranes: 2. Testing the “Two-States” Model of Receptor Activation

2001 • 14 citations