Lifting the lid on GPCRs: the role of extracellular loops

Molecular Basis of Secretin Docking to Its Intact Receptor Using Multiple Photolabile Probes Distributed throughout the Pharmacophore

(2011) Maoqing Dong et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Refinement of Glucagon-like Peptide 1 Docking to Its Intact Receptor Using Mid-region Photolabile Probes and Molecular Modeling

(2011) Laurence J. Miller et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

(2011) Guillaume Lebon et al.   NATURE

Structure of the human histamine H1 receptor complex with doxepin

(2011) Tatsuro Shimamura et al.   NATURE

Crystal structure of metarhodopsin II

(2011) Hui-Woog Choe et al.   NATURE

The structural basis of agonist-induced activation in constitutively active rhodopsin

(2011) Jörg Standfuss et al.   NATURE

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

(2011) Tony Warne et al.   NATURE

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Structure and function of an irreversible agonist-β2 adrenoceptor complex

(2011) Daniel M. Rosenbaum et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Two distinct conformations of helix 6 observed in antagonist-bound structures of a  1-adrenergic receptor

(2011) R. Moukhametzianov et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Successful prediction of the intra- and extracellular loops of four G-protein-coupled receptors

(2011) D. A. Goldfeld et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

Elucidation of the active conformation of the amino terminus of receptor-bound secretin using intramolecular disulfide bond constraints

(2010) Maoqing Dong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structural Insights into Conformational Stability of Wild-Type and Mutant β1-Adrenergic Receptor

(2010) Gouthaman S. Balaraman et al.   BIOPHYSICAL JOURNAL

GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor

(2010) Miriam C. Peeters et al.   FASEB JOURNAL

Third Extracellular Loop (EC3)-N Terminus Interaction Is Important for Seven-transmembrane Domain Receptor Function

(2010) Soumendra Rana et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Secretin Occupies a Single Protomer of the Homodimeric Secretin Receptor Complex

(2010) Maoqing Dong et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Determinants of Allosteric Agonism and Modulation at the M4Muscarinic Acetylcholine Receptor

(2010) Vindhya Nawaratne et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ligand-specific Conformation of Extracellular Loop-2 in the Angiotensin II Type 1 Receptor

(2010) Hamiyet Unal et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Amino-Terminus of Angiotensin II Contacts Several Ectodomains of the Angiotensin II Receptor AT1

(2010) Dany Fillion et al.   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of Disease-Linked Rhodopsin Mutations Based on Structure, Function, and Protein Stability Calculations

(2010) Elizabeth P. Rakoczy et al.   JOURNAL OF MOLECULAR BIOLOGY

Conserved Binding Mode of Human β2Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography

(2010) Daniel Wacker et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Evidence that Interaction between Conserved Residues in Transmembrane Helices 2, 3, and 7 Are Crucial for Human VPAC1 Receptor Activation

(2010) A. O. Chugunov et al.   MOLECULAR PHARMACOLOGY

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor

(2010) Michael P. Bokoch et al.   NATURE

Refinement of the pharmacophore of an agonist ligand of the secretin receptor using conformationally constrained cyclic hexapeptides

(2010) Maoqing Dong et al.   PEPTIDES

Highly conserved tyrosine stabilizes the active state of rhodopsin

(2010) J. A. Goncalves et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

The minor binding pocket: a major player in 7TM receptor activation

(2010) Mette M. Rosenkilde et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Regulation of signal transduction by calcitonin gene-related peptide receptors

(2010) Christopher S Walker et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation

(2010) M.C. Peeters et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Targeting V1A-vasopressin receptors with [Arg6, D-Trp7,9, NmePhe8]-substance P (6-11) identifies a strategy to develop novel anti-cancer therapies

(2009) Alison C. MacKinnon et al.   BRITISH JOURNAL OF PHARMACOLOGY

Unraveling the Structure and Function of G Protein-Coupled Receptors Through NMR Spectroscopy

(2009) Irina Tikhonova et al.   CURRENT PHARMACEUTICAL DESIGN

Orthosteric/Allosteric Bitopic Ligands: Going Hybrid at GPCRs

(2009) C. Valant et al.   MOLECULAR INTERVENTIONS

Alanine Scanning Mutagenesis of the Second Extracellular Loop of Type 1 Corticotropin-Releasing Factor Receptor Revealed Residues Critical for Peptide Binding

(2009) K. Gkountelias et al.   MOLECULAR PHARMACOLOGY

Community-wide assessment of GPCR structure modelling and ligand docking: GPCR Dock 2008

(2009) Mayako Michino et al.   NATURE REVIEWS DRUG DISCOVERY

Helix movement is coupled to displacement of the second extracellular loop in rhodopsin activation

(2009) Shivani Ahuja et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A  -Arrestin-Biased Agonist of the Parathyroid Hormone Receptor (PTH1R) Promotes Bone Formation Independent of G Protein Activation

(2009) D. Gesty-Palmer et al.   Science Translational Medicine

A G protein-coupled receptor at work: the rhodopsin model

(2009) Klaus Peter Hofmann et al.   TRENDS IN BIOCHEMICAL SCIENCES

Passing the baton in class B GPCRs: peptide hormone activation via helix induction?

(2009) Christoph Parthier et al.   TRENDS IN BIOCHEMICAL SCIENCES

Mapping Peptide Hormone−Receptor Interactions Using a Disulfide-Trapping Approach†

(2008) Paul Monaghan et al.   BIOCHEMISTRY

A Second Disulfide Bridge from the N-Terminal Domain to Extracellular Loop 2 Dampens Receptor Activity in GPR39†

(2008) Laura Storjohann et al.   BIOCHEMISTRY

Two Arginine-Glutamate Ionic Locks Near the Extracellular Surface of FFAR1 Gate Receptor Activation

(2008) Chi Shing Sum et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Involvement of the Second Extracellular Loop and Transmembrane Residues of CCR5 in Inhibitor Binding and HIV-1 Fusion: Insights into the Mechanism of Allosteric Inhibition

(2008) Kenji Maeda et al.   JOURNAL OF MOLECULAR BIOLOGY

Conformational Changes in the Parathyroid Hormone Receptor Associated with Activation by Agonist

(2008) Beena E. Thomas et al.   MOLECULAR ENDOCRINOLOGY

Spatial Approximation between Secretin Residue Five and the Third Extracellular Loop of Its Receptor Provides New Insight into the Molecular Basis of Natural Agonist Binding

(2008) M. Dong et al.   MOLECULAR PHARMACOLOGY

Structure of a β1-adrenergic G-protein-coupled receptor

(2008) Tony Warne et al.   NATURE

Crystal structure of opsin in its G-protein-interacting conformation

(2008) Patrick Scheerer et al.   NATURE

Crystal structure of the ligand-free G-protein-coupled receptor opsin

(2008) Jung Hee Park et al.   NATURE

Angiotensin receptor agonistic autoantibodies induce pre-eclampsia in pregnant mice

(2008) Cissy C Zhou et al.   NATURE MEDICINE

Structural diversity of G protein-coupled receptors and significance for drug discovery

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

A Specific Cholesterol Binding Site Is Established by the 2.8 Å Structure of the Human β2-Adrenergic Receptor

(2008) Michael A. Hanson et al.   STRUCTURE

Class-B GPCR activation: is ligand helix-capping the key?

(2008) Jean-Michel Neumann et al.   TRENDS IN BIOCHEMICAL SCIENCES

Heterotrimeric G protein activation by G-protein-coupled receptors

(2007) William M. Oldham et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY