Ligand-specific interactions modulate kinetic, energetic, and mechanical properties of the human β2 adrenergic receptor.

PubWeight™: 1.85‹?› | Rank: Top 3%

🔗 View Article (PMC 4506644)

Published in Structure on June 28, 2012

Authors

Michael Zocher1, Juan J Fung, Brian K Kobilka, Daniel J Müller

Author Affiliations

1: Department of Biosystems Science and Engineering, ETH Zürich, Mattenstr. 26, 4058 Basel, Switzerland.

Articles citing this

Imaging G protein-coupled receptors while quantifying their ligand-binding free-energy landscape. Nat Methods (2015) 1.55

Observing a lipid-dependent alteration in single lactose permeases. Structure (2015) 1.48

Cholesterol increases kinetic, energetic, and mechanical stability of the human β2-adrenergic receptor. Proc Natl Acad Sci U S A (2012) 1.09

Conformational flexibility and structural dynamics in GPCR-mediated G protein activation: a perspective. J Mol Biol (2013) 1.05

Grand opening of structure-guided design for novel opioids. Trends Pharmacol Sci (2012) 1.04

Minireview: More than just a hammer: ligand "bias" and pharmaceutical discovery. Mol Endocrinol (2014) 1.04

Development and characterization of pepducins as Gs-biased allosteric agonists. J Biol Chem (2014) 0.98

Kinetic, energetic, and mechanical differences between dark-state rhodopsin and opsin. Structure (2013) 0.95

P23H opsin knock-in mice reveal a novel step in retinal rod disc morphogenesis. Hum Mol Genet (2013) 0.93

Ligands raise the constraint that limits constitutive activation in G protein-coupled opioid receptors. J Biol Chem (2013) 0.86

Atomic force microscopy: a multifaceted tool to study membrane proteins and their interactions with ligands. Biochim Biophys Acta (2013) 0.86

Substrate-induced changes in the structural properties of LacY. Proc Natl Acad Sci U S A (2014) 0.86

Identifying and quantifying two ligand-binding sites while imaging native human membrane receptors by AFM. Nat Commun (2015) 0.84

Ligand-selective activation of heterologously-expressed mammalian olfactory receptor. Cell Calcium (2014) 0.83

Peptide transporter DtpA has two alternate conformations, one of which is promoted by inhibitor binding. Proc Natl Acad Sci U S A (2013) 0.82

Ligands stabilize specific GPCR conformations: but how? Structure (2012) 0.81

Simulations of biased agonists in the β(2) adrenergic receptor with accelerated molecular dynamics. Biochemistry (2013) 0.81

Detailed analysis of biased histamine H₄ receptor signalling by JNJ 7777120 analogues. Br J Pharmacol (2013) 0.81

Divergent label-free cell phenotypic pharmacology of ligands at the overexpressed β₂-adrenergic receptors. Sci Rep (2014) 0.80

Identification of a Novel Gnao-Mediated Alternate Olfactory Signaling Pathway in Murine OSNs. Front Cell Neurosci (2016) 0.79

Dynamic single-molecule force spectroscopy of rhodopsin in native membranes. Methods Mol Biol (2015) 0.78

Molecular modeling studies give hint for the existence of a symmetric hβ₂R-Gαβγ-homodimer. J Mol Model (2013) 0.77

Retinal Conformation Changes Rhodopsin's Dynamic Ensemble. Biophys J (2015) 0.76

Advances in receptor conformation research: the quest for functionally selective conformations focusing on the β2 -adrenoceptor. Br J Pharmacol (2015) 0.76

Structural approaches to understanding retinal proteins needed for vision. Curr Opin Cell Biol (2013) 0.76

Watching cellular machinery in action, one molecule at a time. J Cell Biol (2016) 0.75

The Allostery Landscape: Quantifying Thermodynamic Couplings in Biomolecular Systems. J Chem Theory Comput (2016) 0.75

Construction of Structural Mimetics of the Thyrotropin Receptor Intracellular Domain. Biophys J (2016) 0.75

Agonist binding by the β2-adrenergic receptor: an effect of receptor conformation on ligand association-dissociation characteristics. Eur Biophys J (2015) 0.75

Olfactory Receptors Modulate Physiological Processes in Human Airway Smooth Muscle Cells. Front Physiol (2016) 0.75

Effect of material flexibility on the thermodynamics and kinetics of hydrophobically induced evaporation of water. Proc Natl Acad Sci U S A (2017) 0.75

G Protein-Coupled Receptors Contain Two Conserved Packing Clusters. Biophys J (2017) 0.75

Articles cited by this

High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science (2007) 20.32

Entropic elasticity of lambda-phage DNA. Science (1994) 15.40

Dynamic strength of molecular adhesion bonds. Biophys J (1997) 14.93

Crystal structure of the human beta2 adrenergic G-protein-coupled receptor. Nature (2007) 14.06

Structure of a beta1-adrenergic G-protein-coupled receptor. Nature (2008) 11.97

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function. Science (2007) 11.74

The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science (2008) 11.74

Transduction of receptor signals by beta-arrestins. Science (2005) 9.87

Structure of a nanobody-stabilized active state of the β(2) adrenoceptor. Nature (2011) 9.61

Crystal structure of opsin in its G-protein-interacting conformation. Nature (2008) 8.61

The structure and function of G-protein-coupled receptors. Nature (2009) 8.08

Probing the relation between force--lifetime--and chemistry in single molecular bonds. Annu Rev Biophys Biomol Struct (2001) 7.19

Structure and function of an irreversible agonist-β(2) adrenoceptor complex. Nature (2011) 5.35

Conformational complexity of G-protein-coupled receptors. Trends Pharmacol Sci (2007) 5.18

Crystal structure of metarhodopsin II. Nature (2011) 5.05

Organization of the G protein-coupled receptors rhodopsin and opsin in native membranes. J Biol Chem (2003) 3.90

The structural basis of agonist-induced activation in constitutively active rhodopsin. Nature (2011) 3.79

Folding and binding cascades: dynamic landscapes and population shifts. Protein Sci (2000) 3.74

Activation of the beta 2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6. J Biol Chem (2001) 3.49

Effect of carboxylic acid side chains on the absorption maximum of visual pigments. Science (1989) 3.44

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor. Nature (2010) 3.19

Dopamine D2 receptors form higher order oligomers at physiological expression levels. EMBO J (2008) 2.99

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex. Proc Natl Acad Sci U S A (2009) 2.86

The forgotten serine. A critical role for Ser-2035.42 in ligand binding to and activation of the beta 2-adrenergic receptor. J Biol Chem (2000) 2.67

Exploring the energy landscape of GFP by single-molecule mechanical experiments. Proc Natl Acad Sci U S A (2004) 2.65

Agonist-induced conformational changes in the G-protein-coupling domain of the beta 2 adrenergic receptor. Proc Natl Acad Sci U S A (2001) 2.58

Dynamics of unfolded polypeptide chains as model for the earliest steps in protein folding. J Mol Biol (2003) 2.56

Energy landscapes of biomolecular adhesion and receptor anchoring at interfaces explored with dynamic force spectroscopy. Faraday Discuss (1998) 2.46

Anisotropic deformation response of single protein molecules. Proc Natl Acad Sci U S A (2006) 2.28

G-protein-coupled receptors: molecular mechanisms involved in receptor activation and selectivity of G-protein recognition. FASEB J (1997) 2.25

Energy landscapes as a tool to integrate GPCR structure, dynamics, and function. Physiology (Bethesda) (2010) 2.05

Ligand-regulated oligomerization of beta(2)-adrenoceptors in a model lipid bilayer. EMBO J (2009) 1.86

Efficacy at G-protein-coupled receptors. Nat Rev Drug Discov (2002) 1.76

Stability of bacteriorhodopsin alpha-helices and loops analyzed by single-molecule force spectroscopy. Biophys J (2002) 1.60

Atomic force microscopy and spectroscopy of native membrane proteins. Nat Protoc (2007) 1.46

Structural insights into adrenergic receptor function and pharmacology. Trends Pharmacol Sci (2011) 1.42

Beta-adrenoceptors on smooth muscle, nerves and inflammatory cells. Life Sci (1993) 1.39

Probing the energy landscape of the membrane protein bacteriorhodopsin. Structure (2004) 1.30

Catecholamine receptors: structure, function, and regulation. Recent Prog Horm Res (1993) 1.30

Beta 2 adrenergic receptors in asthma: a current perspective. Lung (1992) 1.25

Deciphering molecular interactions of native membrane proteins by single-molecule force spectroscopy. Annu Rev Biophys Biomol Struct (2007) 1.18

Locating ligand binding and activation of a single antiporter. EMBO Rep (2005) 1.15

Detecting molecular interactions that stabilize native bovine rhodopsin. J Mol Biol (2006) 1.11

Characterizing molecular interactions in different bacteriorhodopsin assemblies by single-molecule force spectroscopy. J Mol Biol (2005) 1.04

Point mutations in membrane proteins reshape energy landscape and populate different unfolding pathways. J Mol Biol (2007) 1.02

Locating an extracellular K+-dependent interaction site that modulates betaine-binding of the Na+-coupled betaine symporter BetP. Proc Natl Acad Sci U S A (2011) 1.00

Mechanical properties of bovine rhodopsin and bacteriorhodopsin: possible roles in folding and function. Langmuir (2008) 0.99

Structural basis for activation of G-protein-coupled receptors. Pharmacol Toxicol (2002) 0.95

Pharmacological onomastics: what's in a name? Br J Pharmacol (2007) 0.95

Conservation of molecular interactions stabilizing bovine and mouse rhodopsin. Biochemistry (2010) 0.93

Transmembrane helices have rough energy surfaces. J Am Chem Soc (2007) 0.93

From valleys to ridges: exploring the dynamic energy landscape of single membrane proteins. Chemphyschem (2008) 0.91

Substrate binding tunes conformational flexibility and kinetic stability of an amino acid antiporter. J Biol Chem (2009) 0.89

Probing the interactions of carboxy-atractyloside and atractyloside with the yeast mitochondrial ADP/ATP carrier. Structure (2010) 0.88

Detecting molecular interactions that stabilize, activate and guide ligand-binding of the sodium/proton antiporter MjNhaP1 from Methanococcus jannaschii. J Struct Biol (2007) 0.86

Role of extracellular glutamic acids in the stability and energy landscape of bacteriorhodopsin. Biophys J (2008) 0.85

Examining the dynamic energy landscape of an antiporter upon inhibitor binding. J Mol Biol (2007) 0.84

Articles by these authors

High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science (2007) 20.32

Crystal structure of the human beta2 adrenergic G-protein-coupled receptor. Nature (2007) 14.06

Crystal structure of the β2 adrenergic receptor-Gs protein complex. Nature (2011) 13.92

GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function. Science (2007) 11.74

Structure of a nanobody-stabilized active state of the β(2) adrenoceptor. Nature (2011) 9.61

The structure and function of G-protein-coupled receptors. Nature (2009) 8.08

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist. Nature (2012) 6.18

Structure and function of an irreversible agonist-β(2) adrenoceptor complex. Nature (2011) 5.35

betaAR signaling required for diet-induced thermogenesis and obesity resistance. Science (2002) 4.47

The dynamic process of β(2)-adrenergic receptor activation. Cell (2013) 4.09

Structure and dynamics of the M3 muscarinic acetylcholine receptor. Nature (2012) 3.83

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist. Nature (2012) 3.83

Structure of the δ-opioid receptor bound to naltrindole. Nature (2012) 3.69

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor. Nature (2010) 3.19

Linkage of beta1-adrenergic stimulation to apoptotic heart cell death through protein kinase A-independent activation of Ca2+/calmodulin kinase II. J Clin Invest (2003) 3.15

Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational states. J Biol Chem (2003) 2.68

Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature (2013) 2.49

Structure-based discovery of beta2-adrenergic receptor ligands. Proc Natl Acad Sci U S A (2009) 2.48

High-resolution crystal structure of human protease-activated receptor 1. Nature (2012) 2.44

Conformational changes in the G protein Gs induced by the β2 adrenergic receptor. Nature (2011) 2.43

Structure of active β-arrestin-1 bound to a G-protein-coupled receptor phosphopeptide. Nature (2013) 2.14

Depression, antidepressants, and bone health in older adults: a systematic review. J Am Geriatr Soc (2014) 2.08

Energy landscapes as a tool to integrate GPCR structure, dynamics, and function. Physiology (Bethesda) (2010) 2.05

Structure of the rhodopsin dimer: a working model for G-protein-coupled receptors. Curr Opin Struct Biol (2006) 2.03

Structural flexibility of the G alpha s alpha-helical domain in the beta2-adrenoceptor Gs complex. Proc Natl Acad Sci U S A (2011) 2.03

Counting low-copy number proteins in a single cell. Science (2007) 2.01

Antithetic regulation by beta-adrenergic receptors of Gq receptor signaling via phospholipase C underlies the airway beta-agonist paradox. J Clin Invest (2003) 1.87

Ligand-regulated oligomerization of beta(2)-adrenoceptors in a model lipid bilayer. EMBO J (2009) 1.86

Electrostatic cell-surface repulsion initiates lumen formation in developing blood vessels. Curr Biol (2010) 1.83

Myocyte adrenoceptor signaling pathways. Science (2003) 1.81

Nanobody stabilization of G protein-coupled receptor conformational states. Curr Opin Struct Biol (2011) 1.75

Structure-based drug screening for G-protein-coupled receptors. Trends Pharmacol Sci (2012) 1.72

A monoclonal antibody for G protein-coupled receptor crystallography. Nat Methods (2007) 1.60

Dosage-dependent switch from G protein-coupled to G protein-independent signaling by a GPCR. EMBO J (2006) 1.56

Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation. Nature (2016) 1.55

Multiparametric imaging of biological systems by force-distance curve-based AFM. Nat Methods (2013) 1.55

Alignment and cell-matrix interactions of human corneal endothelial cells on nanostructured collagen type I matrices. Invest Ophthalmol Vis Sci (2010) 1.52

The role of ligands on the equilibria between functional states of a G protein-coupled receptor. J Am Chem Soc (2013) 1.48

Imaging and manipulation of biological structures with the AFM. Micron (2002) 1.46

Five challenges to bringing single-molecule force spectroscopy into living cells. Nat Methods (2011) 1.45

Analyzing focal adhesion structure by atomic force microscopy. J Cell Sci (2005) 1.43

Assembly of collagen into microribbons: effects of pH and electrolytes. J Struct Biol (2004) 1.35

Probing the energy landscape of the membrane protein bacteriorhodopsin. Structure (2004) 1.30

A size barrier limits protein diffusion at the cell surface to generate lipid-rich myelin-membrane sheets. Dev Cell (2011) 1.28

Molecular force modulation spectroscopy revealing the dynamic response of single bacteriorhodopsins. Biophys J (2004) 1.28

Unfolding pathways of native bacteriorhodopsin depend on temperature. EMBO J (2003) 1.27

Hydrodynamic effects in fast AFM single-molecule force measurements. Eur Biophys J (2004) 1.23

Structural insights into G-protein-coupled receptor activation. Curr Opin Struct Biol (2008) 1.22

Controlled unfolding and refolding of a single sodium-proton antiporter using atomic force microscopy. J Mol Biol (2004) 1.22

Differential cardioprotective/cardiotoxic effects mediated by beta-adrenergic receptor subtypes. Am J Physiol Heart Circ Physiol (2005) 1.21

Skeletal muscle hypertrophy and anti-atrophy effects of clenbuterol are mediated by the beta2-adrenergic receptor. Muscle Nerve (2002) 1.20

Association between common variants near the melanocortin 4 receptor gene and severe antipsychotic drug-induced weight gain. Arch Gen Psychiatry (2012) 1.20

Organization of beta-adrenoceptor signaling compartments by sympathetic innervation of cardiac myocytes. J Cell Biol (2007) 1.19

Mutation of the alpha2A-adrenoceptor impairs working memory performance and annuls cognitive enhancement by guanfacine. J Neurosci (2002) 1.18

Deciphering molecular interactions of native membrane proteins by single-molecule force spectroscopy. Annu Rev Biophys Biomol Struct (2007) 1.18

A fluorescent probe designed for studying protein conformational change. Proc Natl Acad Sci U S A (2005) 1.17

N-terminal T4 lysozyme fusion facilitates crystallization of a G protein coupled receptor. PLoS One (2012) 1.17

A practical guide to quantify cell adhesion using single-cell force spectroscopy. Methods (2013) 1.12

Detecting molecular interactions that stabilize native bovine rhodopsin. J Mol Biol (2006) 1.11

Role of detergents in conformational exchange of a G protein-coupled receptor. J Biol Chem (2012) 1.10

Cholesterol increases kinetic, energetic, and mechanical stability of the human β2-adrenergic receptor. Proc Natl Acad Sci U S A (2012) 1.09

N-ethylmaleimide-sensitive factor regulates beta2 adrenoceptor trafficking and signaling in cardiomyocytes. Mol Pharmacol (2007) 1.06

Conformational dynamics of single G protein-coupled receptors in solution. J Phys Chem B (2011) 1.06

Association between oxytocin receptor gene polymorphisms and self-rated 'empathic concern' in schizophrenia. PLoS One (2012) 1.06

Engineering rotor ring stoichiometries in the ATP synthase. Proc Natl Acad Sci U S A (2012) 1.05

Fourteen protomers compose the oligomer III of the proton-rotor in spinach chloroplast ATP synthase. J Mol Biol (2003) 1.04

Isoflurane and nociception: spinal alpha2A adrenoceptors mediate antinociception while supraspinal alpha1 adrenoceptors mediate pronociception. Anesthesiology (2002) 1.04

Polymorphisms of the HTR2C gene and antipsychotic-induced weight gain: an update and meta-analysis. Pharmacogenomics (2010) 1.04

Pharmacogenetics of antipsychotics. Can J Psychiatry (2014) 1.02

Determining molecular forces that stabilize human aquaporin-1. J Struct Biol (2003) 1.00

Isolation and characterization of gap junctions from tissue culture cells. J Mol Biol (2002) 0.99

A common polymorphism in the cannabinoid receptor 1 (CNR1) gene is associated with antipsychotic-induced weight gain in Schizophrenia. Neuropsychopharmacology (2010) 0.99

Heterozygous alpha 2A-adrenergic receptor mice unveil unique therapeutic benefits of partial agonists. Proc Natl Acad Sci U S A (2002) 0.99

Regulation of β2-adrenergic receptor function by conformationally selective single-domain intrabodies. Mol Pharmacol (2013) 0.98

Pharmacogenomic testing for neuropsychiatric drugs: current status of drug labeling, guidelines for using genetic information, and test options. Pharmacotherapy (2014) 0.98

Association study of 12 polymorphisms spanning the dopamine D(2) receptor gene and clozapine treatment response in two treatment refractory/intolerant populations. Psychopharmacology (Berl) (2005) 0.97

Probing origins of molecular interactions stabilizing the membrane proteins halorhodopsin and bacteriorhodopsin. Structure (2005) 0.97

Effect of targeted deletions of beta1- and beta2-adrenergic-receptor subtypes on heart rate variability. Am J Physiol Heart Circ Physiol (2005) 0.96

Neurexin-1 and frontal lobe white matter: an overlapping intermediate phenotype for schizophrenia and autism spectrum disorders. PLoS One (2011) 0.96

A new class of amphiphiles bearing rigid hydrophobic groups for solubilization and stabilization of membrane proteins. Chemistry (2012) 0.96

Kinetic, energetic, and mechanical differences between dark-state rhodopsin and opsin. Structure (2013) 0.95

The fuzzy coat of pathological human Tau fibrils is a two-layered polyelectrolyte brush. Proc Natl Acad Sci U S A (2012) 0.94

Fully automated single-molecule force spectroscopy for screening applications. Nanotechnology (2008) 0.94

Wedged AFM-cantilevers for parallel plate cell mechanics. Methods (2013) 0.93

Conservation of molecular interactions stabilizing bovine and mouse rhodopsin. Biochemistry (2010) 0.93

Modulation of molecular interactions and function by rhodopsin palmitylation. Biochemistry (2009) 0.93

Allosteric coupling from G protein to the agonist-binding pocket in GPCRs. Nature (2016) 0.92

Tracking mechanics and volume of globular cells with atomic force microscopy using a constant-height clamp. Nat Protoc (2012) 0.91

From valleys to ridges: exploring the dynamic energy landscape of single membrane proteins. Chemphyschem (2008) 0.91

Single-molecule force spectroscopy from nanodiscs: an assay to quantify folding, stability, and interactions of native membrane proteins. ACS Nano (2011) 0.91

Deciphering teneurin domains that facilitate cellular recognition, cell-cell adhesion, and neurite outgrowth using atomic force microscopy-based single-cell force spectroscopy. Nano Lett (2013) 0.90

Identification and structure of a putative Ca2+-binding domain at the C terminus of AQP1. J Mol Biol (2002) 0.90

Gating of the MlotiK1 potassium channel involves large rearrangements of the cyclic nucleotide-binding domains. Proc Natl Acad Sci U S A (2011) 0.90

Stimulated single-cell force spectroscopy to quantify cell adhesion receptor crosstalk. Proteomics (2010) 0.90

Oxytocin and oxytocin receptor gene polymorphisms and risk for schizophrenia: a case-control study. World J Biol Psychiatry (2012) 0.89

Nanomechanical properties of proteins and membranes depend on loading rate and electrostatic interactions. ACS Nano (2013) 0.89

The intersection of pharmacology, imaging, and genetics in the development of personalized medicine. Dialogues Clin Neurosci (2009) 0.89

Imaging the electrostatic potential of transmembrane channels: atomic probe microscopy of OmpF porin. Biophys J (2002) 0.89

Association of HTR2C, but not LEP or INSIG2, genes with antipsychotic-induced weight gain in a German sample. Pharmacogenomics (2010) 0.88