- Home
- Publications
- Publication Search
- Publication Details
Title
Quantitative structural assessment of graded receptor agonism
Authors
Keywords
-
Journal
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
Volume 116, Issue 44, Pages 22179-22188
Publisher
Proceedings of the National Academy of Sciences
Online
2019-10-15
DOI
10.1073/pnas.1909016116
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- NMR analysis of GPCR conformational landscapes and dynamics
- (2019) Marina Casiraghi et al. MOLECULAR AND CELLULAR ENDOCRINOLOGY
- Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone
- (2019) Sarah A. Mosure et al. JOURNAL OF MEDICINAL CHEMISTRY
- Allosteric Coupling of Drug Binding and Intracellular Signaling in the A 2A Adenosine Receptor
- (2018) Matthew T. Eddy et al. CELL
- Defining a conformational ensemble that directs activation of PPARγ
- (2018) Ian M. Chrisman et al. Nature Communications
- Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation
- (2018) Antonio Laghezza et al. JOURNAL OF MEDICINAL CHEMISTRY
- The nuclear receptor superfamily: A structural perspective
- (2018) Emily R. Weikum et al. PROTEIN SCIENCE
- A2A adenosine receptor functional states characterized by 19F-NMR
- (2018) Lukas Sušac et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Cooperative cobinding of synthetic and natural ligands to the nuclear receptor PPARγ
- (2018) Jinsai Shang et al. eLife
- A Scale of Agonism and Allosteric Modulation for Assessment of Selectivity, Bias, and Receptor Mutation
- (2017) Terry Kenakin MOLECULAR PHARMACOLOGY
- Insight into partial agonism by observing multiple equilibria for ligand-bound and Gs-mimetic nanobody-bound β1-adrenergic receptor
- (2017) Andras S. Solt et al. Nature Communications
- Ligand modulation of sidechain dynamics in a wild-type human GPCR
- (2017) Lindsay D Clark et al. eLife
- Structures of PPARγ complexed with lobeglitazone and pioglitazone reveal key determinants for the recognition of antidiabetic drugs
- (2017) Min A Lee et al. Scientific Reports
- Probing the Complex Binding Modes of the PPARγ Partial Agonist 2-Chloro-N-(3-chloro-4-((5-chlorobenzo[d]thiazol-2-yl)thio)phenyl)-4-(trifluoromethyl)benzenesulfonamide (T2384) to Orthosteric and Allosteric Sites with NMR Spectroscopy
- (2016) Travis S. Hughes et al. JOURNAL OF MEDICINAL CHEMISTRY
- Backbone NMR reveals allosteric signal transduction networks in the β1-adrenergic receptor
- (2016) Shin Isogai et al. NATURE
- Activation of the A2A adenosine G-protein-coupled receptor by conformational selection
- (2016) Libin Ye et al. NATURE
- Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation
- (2016) Dean P. Staus et al. NATURE
- Mechanistic elucidation guided by covalent inhibitors for the development of anti-diabetic PPARγ ligands
- (2016) Hwan Bae et al. Chemical Science
- NMR Methods to Study Dynamic Allostery
- (2016) Sarina Grutsch et al. PLoS Computational Biology
- Identification of a Conformational Equilibrium That Determines the Efficacy and Functional Selectivity of the μ-Opioid Receptor
- (2015) Junya Okude et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Structural Insights into the Dynamic Process of β 2 -Adrenergic Receptor Signaling
- (2015) Aashish Manglik et al. CELL
- Tactical Approaches to Interconverting GPCR Agonists and Antagonists
- (2015) Peter I. Dosa et al. JOURNAL OF MEDICINAL CHEMISTRY
- Propagation of conformational changes during μ-opioid receptor activation
- (2015) Rémy Sounier et al. NATURE
- Pharmacological repression of PPARγ promotes osteogenesis
- (2015) David P. Marciano et al. Nature Communications
- Mapping the conformational landscape of a dynamic enzyme by multitemperature and XFEL crystallography
- (2015) Daniel A Keedy et al. eLife
- Functional Dynamics of Deuterated β2-Adrenergic Receptor in Lipid Bilayers Revealed by NMR Spectroscopy
- (2014) Yutaka Kofuku et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- What is pharmacological ‘affinity’? Relevance to biased agonism and antagonism
- (2014) Terry Kenakin TRENDS IN PHARMACOLOGICAL SCIENCES
- An alternate binding site for PPARγ ligands
- (2014) Travis S. Hughes et al. Nature Communications
- The Dynamic Process of β2-Adrenergic Receptor Activation
- (2013) Rie Nygaard et al. CELL
- The Role of Ligands on the Equilibria Between Functional States of a G Protein-Coupled Receptor
- (2013) Tae Hun Kim et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Allostery and the Monod-Wyman-Changeux Model After 50 Years
- (2012) Jean-Pierre Changeux Annual Review of Biophysics
- Subtleties in GPCR drug discovery: a medicinal chemistry perspective
- (2012) Masahiko Fujioka et al. DRUG DISCOVERY TODAY
- Evidence for dynamics in proteins as a mechanism for ligand dissociation
- (2012) Mary J Carroll et al. Nature Chemical Biology
- Low-Resolution Molecular Models Reveal the Oligomeric State of the PPAR and the Conformational Organization of Its Domains in Solution
- (2012) Amanda Bernardes et al. PLoS One
- Medium Chain Fatty Acids Are Selective Peroxisome Proliferator Activated Receptor (PPAR) γ Activators and Pan-PPAR Partial Agonists
- (2012) Marcelo Vizoná Liberato et al. PLoS One
- Biased Signaling Pathways in 2-Adrenergic Receptor Characterized by 19F-NMR
- (2012) J. J. Liu et al. SCIENCE
- Ligand and Receptor Dynamics Contribute to the Mechanism of Graded PPARγ Agonism
- (2012) Travis S. Hughes et al. STRUCTURE
- Efficacy of the β2-adrenergic receptor is determined by conformational equilibrium in the transmembrane region
- (2012) Yutaka Kofuku et al. Nature Communications
- Accessing protein conformational ensembles using room-temperature X-ray crystallography
- (2011) J. S. Fraser et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Allostery and population shift in drug discovery
- (2010) Gozde Kar et al. CURRENT OPINION IN PHARMACOLOGY
- Alternate States of Proteins Revealed by Detailed Energy Landscape Mapping
- (2010) Michael D. Tyka et al. JOURNAL OF MOLECULAR BIOLOGY
- Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor
- (2010) Michael P. Bokoch et al. NATURE
- Hidden alternative structures of proline isomerase essential for catalysis
- (2009) James S. Fraser et al. NATURE
- The role of dynamic conformational ensembles in biomolecular recognition
- (2009) David D Boehr et al. Nature Chemical Biology
Find Funding. Review Successful Grants.
Explore over 25,000 new funding opportunities and over 6,000,000 successful grants.
ExploreDiscover Peeref hubs
Discuss science. Find collaborators. Network.
Join a conversation