Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Conformational rearrangement during activation of a metabotropic glutamate receptor

(2021) Brandon Wey-Hung Liauw et al.   Nature Chemical Biology

Single-molecule FRET imaging of GPCR dimers in living cells

(2021) Wesley B. Asher et al.   NATURE METHODS

Structural basis of GABAB receptor–Gi protein coupling

(2021) Cangsong Shen et al.   NATURE

How do branched detergents stabilize GPCRs in micelles?

(2020) Sangbae Lee et al.   BIOCHEMISTRY

Structural basis of the activation of a metabotropic GABA receptor

(2020) Hamidreza Shaye et al.   NATURE

Structural insights into probe-dependent positive allosterism of the GLP-1 receptor

(2020) Ana B. Bueno et al.   Nature Chemical Biology

Structural insights into the activation initiation of full-length mGlu1

(2020) Jinyi Zhang et al.   Protein & Cell

Structural insights into the activation of metabotropic glutamate receptors

(2019) Antoine Koehl et al.   NATURE

Stepwise activation of a class C GPCR begins with millisecond dimer rearrangement

(2019) Eugene O. Grushevskyi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mechanism of β2AR regulation by an intracellular positive allosteric modulator

(2019) Xiangyu Liu et al.   SCIENCE

Local membrane charge regulates β2 adrenergic receptor coupling to Gi3

(2019) M. J. Strohman et al.   Nature Communications

Rearrangement of the transmembrane domain interfaces associated with the activation of a GPCR hetero-oligomer

(2019) Li Xue et al.   Nature Communications

Studying GPCR conformational dynamics by single molecule fluorescence

(2019) Robert B. Quast et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

PAM: A Framework for Integrated Analysis of Imaging, Single-Molecule, and Ensemble Fluorescence Data

(2018) Waldemar Schrimpf et al.   BIOPHYSICAL JOURNAL

Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures

(2018) John A. Christopher et al.   JOURNAL OF MEDICINAL CHEMISTRY

Differential Pharmacology and Binding of mGlu2Receptor Allosteric Modulators

(2018) Daniel E. O’Brien et al.   MOLECULAR PHARMACOLOGY

Precision and accuracy of single-molecule FRET measurements—a multi-laboratory benchmark study

(2018) Björn Hellenkamp et al.   NATURE METHODS

Chloride ions stabilize the glutamate-induced active state of the metabotropic glutamate receptor 3

(2018) Amélie S. Tora et al.   NEUROPHARMACOLOGY

Structural insights into binding specificity, efficacy and bias of a β2AR partial agonist

(2018) Matthieu Masureel et al.   Nature Chemical Biology

HTS-compatible FRET-based conformational sensors clarify membrane receptor activation

(2017) Pauline Scholler et al.   Nature Chemical Biology

Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders

(2017) Daniel J. Foster et al.   NEURON

Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation

(2017) Pauline Scholler et al.   Nature Communications

Cellular Cholesterol Directly Activates Smoothened in Hedgehog Signaling

(2016) Pengxiang Huang et al.   CELL

Organization and functions of mGlu and GABAB receptor complexes

(2016) Jean-Philippe Pin et al.   NATURE

Mechanism of Assembly and Cooperativity of Homomeric and Heteromeric Metabotropic Glutamate Receptors

(2016) Joshua Levitz et al.   NEURON

Allosteric Binding Site and Activation Mechanism of Class C G-Protein Coupled Receptors: Metabotropic Glutamate Receptor Family

(2015) Zhiwei Feng et al.   AAPS Journal

Superagonism at G protein-coupled receptors and beyond

(2015) R Schrage et al.   BRITISH JOURNAL OF PHARMACOLOGY

Overlapping binding sites drive allosteric agonism and positive cooperativity in type 4 metabotropic glutamate receptors

(2015) Xavier Rovira et al.   FASEB JOURNAL

Conformational dynamics of a class C G-protein-coupled receptor

(2015) Reza Vafabakhsh et al.   NATURE

High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875

(2014) Ankita Srivastava et al.   NATURE

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

(2014) Andrew S. Doré et al.   NATURE

Major ligand-induced rearrangement of the heptahelical domain interface in a GPCR dimer

(2014) Li Xue et al.   Nature Chemical Biology

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

(2014) H. Wu et al.   SCIENCE

Fine tuning of sub-millisecond conformational dynamics controls metabotropic glutamate receptors agonist efficacy

(2014) Linnea Olofsson et al.   Nature Communications

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors

(2013) E. Doumazane et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Unique Signaling Profiles of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Determine Differences in In Vivo Activity

(2012) Jerri M. Rook et al.   BIOLOGICAL PSYCHIATRY

A New Class of Amphiphiles Bearing Rigid Hydrophobic Groups for Solubilization and Stabilization of Membrane Proteins

(2012) Pil Seok Chae et al.   CHEMISTRY-A EUROPEAN JOURNAL

Combining MFD and PIE for Accurate Single-Pair Förster Resonance Energy Transfer Measurements

(2012) Volodymyr Kudryavtsev et al.   CHEMPHYSCHEM

GPCR stabilization using the bicelle-like architecture of mixed sterol-detergent micelles

(2011) Aaron A. Thompson et al.   METHODS

FRET Efficiency Distributions of Multistate Single Molecules

(2010) Irina V. Gopich et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Positive allosteric modulators of the human sweet taste receptor enhance sweet taste

(2010) G. Servant et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum et al.   NATURE

Optical measurement of mGluR1 conformational changes reveals fast activation, slow deactivation, and sensitization

(2009) P. Marcaggi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

(2009) X. J. Yao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

Molecular mechanism for the umami taste synergism

(2008) F. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA