The Molecular Basis of G Protein–Coupled Receptor Activation

Crystal Structure of Rhodopsin: A G Protein-Coupled Receptor

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High-Resolution Crystal Structure of an Engineered Human β 2 -Adrenergic G Protein–Coupled Receptor

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The Energy Landscapes and Motions of Proteins

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Crystal structure of the β2 adrenergic receptor–Gs protein complex

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[19] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors

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The G-Protein-Coupled Receptors in the Human Genome Form Five Main Families. Phylogenetic Analysis, Paralogon Groups, and Fingerprints

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Dynamic personalities of proteins

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Crystal structure of the human β2 adrenergic G-protein-coupled receptor

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

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GPR132 regulates the function of NK cells through the Gαs/CSK/ZAP70/NF-κB signaling pathway as a potential immune checkpoint

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Hot spots for GPCR signaling: lessons from single-molecule microscopy

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Role of Actin Cytoskeleton in Dynamics and Function of the Serotonin1A Receptor

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Supporting individuals using medications for opioid use disorder in recovery residences: challenges and opportunities for addressing the opioid epidemic

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Structural insights into ligand recognition and activation of angiotensin receptors

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In Silico Identification of Cholesterol Binding Motifs in the Chemokine Receptor CCR3

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Deconstructing the transmembrane core of class A G protein–coupled receptors

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Recent Advances in Structure, Function, and Pharmacology of Class A Lipid GPCRs: Opportunities and Challenges for Drug Discovery

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Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of Adhesion Receptor GPR97

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Systematic identification and functional characterization of the CFEM proteins in poplar fungus Marssonina brunnea

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Physiological changes in bilayer thickness induced by cholesterol control GPCR rhodopsin function

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The role of G protein-coupled receptor in neutrophil dysfunction during sepsis-induced acute respiratory distress syndrome

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Cryo-EM structure of the human chemerin receptor 1–Gi protein complex bound to the C-terminal nonapeptide of chemerin

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Structural basis for ligand recognition and signaling of hydroxy-carboxylic acid receptor 2

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International Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors

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Not all arrestins are created equal: Therapeutic implications of the functional diversity of the β arrestins in the heart

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The Effect of Deuteration on the H2 Receptor Histamine Binding Profile: A Computational Insight into Modified Hydrogen Bonding Interactions

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Photoswitch dissociation from a G protein-coupled receptor resolved by time-resolved serial crystallography

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Activation Microswitches in Adenosine Receptor A 2A Function as Rheostats in the Cell Membrane

Ma, N., Lee, S., & Vaidehi, N. (2020) · Biochemistry · doi:10.1021/acs.biochem.0c00626 · Cited by 22

Biased Ligands Differentially Shape the Conformation of the Extracellular Loop Region in 5-HT2B Receptors

Denzinger, K., Nguyen, T. N., Noonan, T., Wolber, G., & Bermúdez, M. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21249728 · Cited by 22

Lipids and Phosphorylation Conjointly Modulate Complex Formation of β2-Adrenergic Receptor and β-arrestin2

Pluháčková, K., Wilhelm, F. M., & Müller, D. J. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.807913 · Cited by 19

Dynamics and mechanistic underpinnings to pharmacology of class A GPCRs: an NMR perspective

Huang, S. K., & Prosser, R. S. (2022) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00044.2022 · Cited by 22

Pharmacological targeting of G protein-coupled receptor heteromers

Moreno, E., Casajuana-Martín, N., Coyle, M., Campos, B., Galaj, E., del Torrent, C. L., Seyedian, A., Rea, W. P., Cai, N.-S., Bonifazi, A., et al. (2022) · Pharmacological Research · doi:10.1016/j.phrs.2022.106476 · Cited by 22

Conformational Dynamics of the Activated GLP-1 Receptor-Gs Complex Revealed by Cross-Linking Mass Spectrometry and Integrative Structure Modeling

Yuan, S., Xia, L., Wang, C., Wu, F., Zhang, B., Pan, C., Fan, Z., Lei, X., Stevens, R. C., Šali, A., et al. (2023) · ACS Central Science · doi:10.1021/acscentsci.3c00063 · Cited by 22

Homo- and hetero-dimeric subunit interactions set affinity and efficacy in metabotropic glutamate receptors

Habrian, C. H., Latorraca, N. R., Fu, Z., & Isacoff, E. Y. (2023) · Nature Communications · doi:10.1038/s41467-023-44013-4 · Cited by 22

Exploring the Activation Mechanism of a Metabotropic Glutamate Receptor Homodimer via Molecular Dynamics Simulation

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Computational Investigations on the Binding Mode of Ligands for the Cannabinoid-Activated G Protein-Coupled Receptor GPR18

Neumann, A., Engel, V., Mahardhika, A. B., Schoeder, C. T., Namasivayam, V., Kieć‐Kononowicz, K., & Müller, C. E. (2020) · Biomolecules · doi:10.3390/biom10050686 · Cited by 23

Structural heterogeneity of the ion and lipid channel TMEM16F

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Functional consequences of spatial, temporal and ligand bias of G protein-coupled receptors

Tóth, A. D., Turu, G., & Hunyady, L. (2024) · Nature Reviews Nephrology · doi:10.1038/s41581-024-00869-3 · Cited by 22

Structural insight into Class F receptors – What have we learnt regarding agonist‐induced activation?

Schulte, G., & Kozielewicz, P. (2019) · Basic & Clinical Pharmacology & Toxicology · doi:10.1111/bcpt.13235 · Cited by 24

The zoospores of the thraustochytrid Aurantiochytrium limacinum : Transcriptional reprogramming and lipid metabolism associated to their specific functions

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C-Graphs Tool with Graphical User Interface to Dissect Conserved Hydrogen-Bond Networks: Applications to Visual Rhodopsins

Bertalan, É., Lesca, E., Schertler, G. F. X., & Bondar, A. (2021) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.1c00827 · Cited by 21

Effect of Ligands and Transducers on the Neurotensin Receptor 1 Conformational Ensemble

Dixon, A. D., Inoue, A., Robson, S. A., Culhane, K. J., Trinidad, J. C., Sivaramakrishnan, S., Bumbak, F., & Ziarek, J. J. (2022) · Journal of the American Chemical Society · doi:10.1021/jacs.2c00828 · Cited by 21

Development of an Allostery Responsive Chromatographic Method for Screening Potential Allosteric Modulator of Beta2-adrenoceptor from a Natural Product-Derived DNA-Encoded Chemical Library

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Optical control of the β2-adrenergic receptor with opto-prop-2: A cis-active azobenzene analog of propranolol

Bosma, R., Dijon, N. C., Zheng, Y., Schihada, H., Hauwert, N. J., Shi, S., Arimont, M., Riemens, R., Custers, H., van de Stolpe, A., et al. (2022) · iScience · doi:10.1016/j.isci.2022.104882 · Cited by 21

Genetically encoded fluorescent biosensors for GPCR research

Kim, H., Baek, I.-Y., & Seong, J. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.1007893 · Cited by 25

Structural basis of G protein–Coupled receptor CMKLR1 activation and signaling induced by a chemerin-derived agonist

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Photochromic peptidic NPY Y 4 receptor ligands

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Insights into Nuclear G-Protein-Coupled Receptors as Therapeutic Targets in Non-Communicable Diseases

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Gβγ translocation to the Golgi apparatus activates ARF1 to spatiotemporally regulate G protein–coupled receptor signaling to MAPK

Khater, M., Bryant, C. N., & Wu, G. (2021) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2021.100805 · Cited by 21

Molecular mechanism of distinct chemokine engagement and functional divergence of the human Duffy antigen receptor

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Structural basis for the ligand recognition and G protein subtype selectivity of kisspeptin receptor

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Metformin and the PI3K/AKT signaling pathway: implications for cancer, cardiovascular, and central nervous system diseases

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The G protein-coupled receptor ADGRG6 maintains mouse growth plate homeostasis through IHH signaling

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Allosteric modulation and biased signalling at free fatty acid receptor 2

Zhang, X., Guseynov, A.-A. D., Jenkins, L., Valentini, A., Marsango, S., Schultz-Knudsen, K., Ulven, T., Ulven, E. R., Tikhonova, I. G., Milligan, G., et al. (2025) · Nature · doi:10.1038/s41586-025-09186-6 · Cited by 20

Striated muscle proteins are regulated both by mechanical deformation and by chemical post-translational modification

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Cardiovascular angiotensin II type 1 receptor biased signaling: Focus on non-Gq-, non-βarrestin-dependent signaling

Lymperopoulos, A., Borges, J. I., Carbone, A. M., Cora, N., & Sizova, A. (2021) · Pharmacological Research · doi:10.1016/j.phrs.2021.105943 · Cited by 20

Stabilization of pre-existing neurotensin receptor conformational states by β-arrestin-1 and the biased allosteric modulator ML314

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Overview of pyroptosis mechanism and in-depth analysis of cardiomyocyte pyroptosis mediated by NF-κB pathway in heart failure

Zhang, Z., Yang, Z., Wang, S., Wang, X., & Mao, J. (2024) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2024.117367 · Cited by 22

Machine Learning for Prioritization of Thermostabilizing Mutations for G-Protein Coupled Receptors

Muk, S., Ghosh, S., Achuthan, S., Chen, X., Yao, X.-J., Sandhu, M., Griffor, M. C., Fennell, K. F., Che, Y., Shanmugasundaram, V., et al. (2019) · Biophysical Journal · doi:10.1016/j.bpj.2019.10.023 · Cited by 19

Orthosteric muscarinic receptor activation by the insect repellent IR3535 opens new prospects in insecticide-based vector control

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Signaling roles of phosphoinositides in the retina

Rajala, R. V. S. (2020) · Journal of Lipid Research · doi:10.1194/jlr.tr120000806 · Cited by 20

Characterization of the Role of a Non-GPCR Membrane-Bound CFEM Protein in the Pathogenicity and Germination of Botrytis cinerea

Arya, G. C., Srivastava, D. A., Pandaranayaka, E. P. J., Manasherova, E., Prusky, D., Elad, Y., Frenkel, O., Dvir, H., & Harel, A. (2020) · Microorganisms · doi:10.3390/microorganisms8071043 · Cited by 22

Function and therapeutic potential of G protein‐coupled receptors in epididymis

Zhang, D., Wang, Y., Lin, H., Sun, Y., Wang, M., Jia, Y., Yu, X., Jiang, H., Xu, W., Sun, J., et al. (2020) · British Journal of Pharmacology · doi:10.1111/bph.15252 · Cited by 22

Principles and Methods in Computational Membrane Protein Design

Vorobieva, A. A. (2021) · Journal of Molecular Biology · doi:10.1016/j.jmb.2021.167154 · Cited by 20

A cellular perspective of bias at G protein‐coupled receptors

Fernández, T. J., Maria, M. D., & Lobingier, B. T. (2020) · Protein Science · doi:10.1002/pro.3872 · Cited by 20

Illuminating the neuropeptide Y4 receptor and its ligand pancreatic polypeptide from a structural, functional, and therapeutic perspective

Schüß, C., Behr, V., & Beck‐Sickinger, A. G. (2024) · Neuropeptides · doi:10.1016/j.npep.2024.102416 · Cited by 19

Targeting adhesion G protein-coupled receptors. Current status and future perspectives

Ließmann, F., von Bredow, L., Meiler, J., & Liebscher, I. (2024) · Structure · doi:10.1016/j.str.2024.10.022 · Cited by 19

Molecular basis of β-arrestin coupling to the metabotropic glutamate receptor mGlu3

Wen, T., Du, M., Lu, Y., Jia, N., Lu, X., Liu, N., Chang, S., Zhang, X., Shen, Y., & Yang, X. (2025) · Nature Chemical Biology · doi:10.1038/s41589-025-01858-8 · Cited by 19

A Conserved Proline Hinge Mediates Helix Dynamics and Activation of Rhodopsin

Pope, A., Sánchez-Reyes, O. B., South, K., Zaitseva, E., Ziliox, M., Vogel, R., Reeves, P. J., & Smith, S. O. (2020) · Structure · doi:10.1016/j.str.2020.05.004 · Cited by 21

Oligopeptides as Neuropeptide Y Y4 Receptor Ligands: Identification of a High-Affinity Tetrapeptide Agonist and a Hexapeptide Antagonist

Konieczny, A., Braun, D., Wifling, D., Bernhardt, G., & Keller, M. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00426 · Cited by 19

Structural insights into the G protein selectivity revealed by the human EP3-Gi signaling complex

Suno, R., Sugita, Y., Morimoto, K., Takazaki, H., Tsujimoto, H., Hirose, M., Suno-Ikeda, C., Nomura, N., Hino, T., Inoue, A., et al. (2022) · Cell Reports · doi:10.1016/j.celrep.2022.111323 · Cited by 20

Targeting in silico GPCR conformations with ultra-large library screening for hit discovery

Sala, D., Batebi, H., Ledwitch, K. V., Hildebrand, P. W., & Meiler, J. (2023) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2022.12.006 · Cited by 20

Discovery and design of G protein-coupled receptor targeting antibodies

Peterson, S. M., Hutchings, C. J., Hu, C. F., Mathur, M., Salameh, J. W., Axelrod, F. T., & Sato, A. K. (2023) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2023.2193389 · Cited by 19

Distinct activation mechanisms regulate subtype selectivity of Cannabinoid receptors

Dutta, S., & Shukla, D. (2023) · Communications Biology · doi:10.1038/s42003-023-04868-1 · Cited by 19

When natural antibodies become pathogenic: autoantibodies targeted against G protein-coupled receptors in the pathogenesis of systemic sclerosis

Akbarzadeh, R., Müller, A., Humrich, J. Y., & Riemekasten, G. (2023) · Frontiers in Immunology · doi:10.3389/fimmu.2023.1213804 · Cited by 19

Presynaptic nanoscale components of retrograde synaptic signaling

Barti, B., Dudok, B., Kenesei, K., Zöldi, M., Miczán, V., Balla, G. Y., Zala, D., Tasso, M., Sagheddu, C., Kisfali, M., et al. (2024) · Science Advances · doi:10.1126/sciadv.ado0077 · Cited by 19

Structure and dynamics of dynorphin peptide and its receptor

Ferré, G., Czaplicki, G., Demange, P., & Milon, A. (2019) · Vitamins and hormones · doi:10.1016/bs.vh.2019.05.006 · Cited by 19

Imaging GPCR internalization using near-infrared Nebraska red-based reagents

Lesiak, L., Zhou, X., Yuan, F., Zhao, J., Beck, J. R., & Stains, C. I. (2020) · Organic & Biomolecular Chemistry · doi:10.1039/d0ob00043d · Cited by 19

Opioid Pharmacology under the Microscope

Jullié, D., Gondin, A. B., von Zastrow, M., & Canals, M. (2020) · Molecular Pharmacology · doi:10.1124/mol.119.119321 · Cited by 17

Atomic-Level Characterization of the Methadone-Stabilized Active Conformation of µ-Opioid Receptor

Kapoor, A., Provasi, D., & Filizola, M. (2020) · Molecular Pharmacology · doi:10.1124/mol.119.119339 · Cited by 19

Agonist Binding and G Protein Coupling in Histamine H2 Receptor: A Molecular Dynamics Study

Conrad, M., Söldner, C. A., Miao, Y., & Sticht, H. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21186693 · Cited by 19

Cyclic Adenosine Monophosphate in Cardiac and Sympathoadrenal GLP-1 Receptor Signaling: Focus on Anti-Inflammatory Effects

Lymperopoulos, A., Borges, J. I., & Stoicovy, R. A. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16060693 · Cited by 18

GPCR signaling via cAMP nanodomains

Yadav, R., & Zaccolo, M. (2025) · Biochemical Journal · doi:10.1042/bcj20253088 · Cited by 18

Butyrate Produced by Gut Microbiota Regulates Atherosclerosis: A Narrative Review of the Latest Findings

Dicks, L. M. T. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26146744 · Cited by 22

The Role of PDE8 in T Cell Recruitment and Function in Inflammation

Epstein, P. M., Basole, C. P., & Brocke, S. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.636778 · Cited by 18

Molecular Insights into Phosphorylation-Induced Allosteric Conformational Changes in a β 2 -Adrenergic Receptor

Madhu, M. K., Debroy, A., & Murarka, R. K. (2022) · The Journal of Physical Chemistry B · doi:10.1021/acs.jpcb.1c08610 · Cited by 18

Evolutionary analyses reveal immune cell receptor GPR84 as a conserved receptor for bacteria-derived molecules

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G Protein-Coupled Receptors Regulated by Membrane Potential

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Small-molecule targeting of GPCR-independent noncanonical G-protein signaling in cancer

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Binding kinetics drive G protein subtype selectivity at the β1-adrenergic receptor

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Multiple recent HCAR2 structures demonstrate a highly dynamic ligand binding and G protein activation mode

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Role of the V2R–βarrestin–Gβγ complex in promoting G protein translocation to endosomes

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GPR50-Ctail cleavage and nuclear translocation: a new signal transduction mode for G protein-coupled receptors

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Transcriptomics analysis reveals potential mechanisms underlying mitochondrial dysfunction and T cell exhaustion in astronauts’ blood cells in space

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Noncanonical interactions of G proteins and β‐arrestins: from competitors to companions

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In Silico Study of Allosteric Communication Networks in GPCR Signaling Bias

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G-Protein Coupled Receptors in Human Sperm: An In Silico Approach to Identify Potential Modulatory Targets

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Structural basis for motilin and erythromycin recognition by motilin receptor

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The ketone body acetoacetate activates human neutrophils through FFAR2

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General Metadynamics Protocol To Simulate Activation/Deactivation of Class A GPCRs: Proof of Principle for the Serotonin Receptor

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Functional Connectome Hierarchy in Schizotypy and Its Associations With Expression of Schizophrenia-Related Genes

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The quest for high-resolution G protein-coupled receptor–G protein structures

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Mechanistic Understanding of Peptide Analogues, DALDA, [Dmt1]DALDA, and KGOP01, Binding to the Mu Opioid Receptor

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Structural Basis for G Protein–Coupled Receptor Signaling

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G protein‐coupled receptors: a count of 1001 conformations

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