Identification of an Efficacy Switch Region in the Ghrelin Receptor Responsible for Interchange between Agonism and Inverse Agonism

Engineering hybrid genes without the use of restriction enzymes: gene splicing by overlap extension

1989 • 3,067 citations

The probable arrangement of the helices in G protein-coupled receptors.

1993 • 977 citations

Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors

2002 • 606 citations

High Constitutive Signaling of the Ghrelin Receptor—Identification of a Potent Inverse Agonist

2003 • 489 citations

Structural basis of β‐adrenergic receptor function

1989 • 480 citations

Activation of rhodopsin: new insights from structural and biochemical studies

2001 • 406 citations

MOLECULAR MECHANISM OF 7TM RECEPTOR ACTIVATION—A GLOBAL TOGGLE SWITCH MODEL

2006 • 397 citations

Loss of constitutive activity of the growth hormone secretagogue receptor in familial short stature

2006 • 335 citations

Common Structural Basis for Constitutive Activity of the Ghrelin Receptor Family

2004 • 335 citations

Sequential Binding of Agonists to the β2 Adrenoceptor

2003 • 333 citations

The Binding Site of Aminergic G Protein–Coupled Receptors: The Transmembrane Segments and Second Extracellular Loop

2002 • 317 citations

Locating ligand-binding sites in 7tm receptors by protein engineering

1994 • 282 citations

Probing the β2 Adrenoceptor Binding Site with Catechol Reveals Differences in Binding and Activation by Agonists and Partial Agonists

2005 • 260 citations

A consensus view of protein dynamics

2007 • 222 citations

Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans

2004 • 199 citations

Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans

2004 • 184 citations

Binding of 125I-labeled ghrelin to membranes from human hypothalamus and pituitary gland

2001 • 167 citations

Specific receptors for synthetic GH secretagogues in the human brain and pituitary gland

1998 • 148 citations

Ghrelin Receptor Gene: Identification of Several Sequence Variants in Extremely Obese Children and Adolescents, Healthy Normal-Weight and Underweight Students, and Children with Short Normal Stature

2004 • 146 citations

Nonpeptide and Peptide Growth Hormone Secretagogues Act Both as Ghrelin Receptor Agonist and as Positive or Negative Allosteric Modulators of Ghrelin Signaling

2005 • 123 citations

Textbook of Receptor Pharmacology

2010 • 123 citations

Ghrelin receptor mutations -- too little height and too much hunger

2006 • 100 citations

Metal Ion Site Engineering Indicates a Global Toggle Switch Model for Seven-transmembrane Receptor Activation

2006 • 92 citations

Ghrelin Receptor Inverse Agonists: Identification of an Active Peptide Core and Its Interaction Epitopes on the Receptor

2006 • 86 citations

Synergistic Contributions of the Functional Groups of Epinephrine to Its Affinity and Efficacy at the β₂Adrenergic Receptor

2004 • 86 citations

Structure−Activity Studies of Orexin A and Orexin B at the Human Orexin 1 and Orexin 2 Receptors Led to Orexin 2 Receptor Selective and Orexin 1 Receptor Preferring Ligands

2004 • 77 citations

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

2001 • 77 citations

Textbook of Receptor Pharmacology

2002 • 71 citations

Disulfide trapping to localize small-molecule agonists and antagonists for a G protein-coupled receptor

2005 • 69 citations

Steric Hindrance Mutagenesis versus Alanine Scan in Mapping of Ligand Binding Sites in the Tachykinin NK₁Receptor

1998 • 66 citations

Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists.

1996 • 62 citations

Identification of an Agonist-induced Conformational Change Occurring Adjacent to the Ligand-binding Pocket of the M3 Muscarinic Acetylcholine Receptor

2005 • 53 citations

Agonist Binding: A Multistep Process: Fig. 1.

2004 • 51 citations

“Induced-Fit” Mechanism for Catecholamine Binding to the β₂-Adrenergic Receptor

2004 • 34 citations

Site-specific Disulfide Capture of Agonist and Antagonist Peptides on the C5a Receptor

2004 • 34 citations

F200A substitution in the third transmembrane helix of human cannabinoid CB1 receptor converts AM2233 from receptor agonist to inverse agonist

2006 • 21 citations

pH Dependence of Photolysis Intermediates in the Photoactivation of Rhodopsin Mutant E113Q

1999 • 16 citations

Novel Mutants of the Human β1-Adrenergic Receptor Reveal Amino Acids Relevant for Receptor Activation

2006 • 9 citations