ArticleNature communications2015
The experimental power of FR900359 to study Gq-regulated biological processes.
Open access · goldAbstract read
In one paragraph
Article in Nature communications, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 221 papers.
0numbers the graph read from it
0cells of the map it votes in
221citing papers in PubMed
11.9field-weighted citation impact, top 1% of its field
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
221 citing papers in PubMed, 360 citations in OpenAlex.
- Inhibitory probes for spatiotemporal analysis of GαNature chemical biology · 2026Article
- Article
- PLCβs are recruited to the plasma membrane in macrophages by both Gβγ and GαProceedings of the National Academy of Sciences of the United States of America · 2026Article
- Does the ERBB/EGF Signaling Network Serve as a Nexus for Oncogenic Signals in Uveal Melanoma?Biomolecules · 2026Review
- Structural determinants of ligand response specificity in the mast cell activating GPCR, MRGPRX2.The Journal of biological chemistry · 2026Article
- TBXA2R activates ERMs to drive motility, invasion, and metastatic colonization of TNBC cells.Life science alliance · 2026Article
- Brain endothelial GαEBioMedicine · 2026Article
- Molecular jackhammers induce intracellular calcium release and skeletal muscle contraction by vibronic-driven action.Chemical science · 2026Article
- Small-molecule inhibitor of Gαo for GNAO1 encephalopathy.Bioscience reports · 2026Article
- Latrophilin-1-Mediated GCells · 2026Article
- Protease-Activated Receptor 1 as an Endogenous Model of Peptidergic Gαq-Gα12-Biased G Protein Signaling.bioRxiv : the preprint server for biology · 2026Article
- TRH can stimulate the release of two POMC-derived pituitary hormones, ACTH and MSH, in medaka.Endocrinology · 2026Article
- PLCβs are recruited to the plasma membrane in macrophages by both Gβγ and GαbioRxiv : the preprint server for biology · 2026Article
- T2R5 Agonist Phendione Decreases Cell Viability and Induces Apoptosis in Head and Neck Squamous Cell Carcinoma.Molecular cancer therapeutics · 2026Article
- Conformational biosensors delineate endosomal G protein regulation by GPCRs.Nature communications · 2026Article
- Mast cell-specific CysLT2 receptor signaling inhibits cysteinyl leukotriene-dependent mast cell activation and type 2 allergic lung inflammation.Cell reports · 2026Article
- Re-evaluating Gα protein-response element specificity in GPCR signaling.Communications biology · 2026Article
- Protease-activated receptor 1 as an endogenous model of peptidergic Gαq-Gα12-biased G protein signaling.Frontiers in molecular biosciences · 2026Article
- Insights into G-protein coupling preference from cryo-EM structures of GNature chemical biology · 2025Article
- Targeting of specific CCR5-G protein complexes underlies biased signaling by HIV-1 envelope glycoproteins.Cell communication and signaling : CCS · 2025Article
161 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
46 authors at 9 institutions in 6 countries.
Ramona SchrageMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Anna-Lena SchmitzMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Evelyn GaffalDepartment of Dermatology and Allergy, Laboratory of Experimental Dermatology, University of Bonn, 53105 Bonn, Germany.
Suvi AnnalaMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Stefan KehrausInstitute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Daniela WenzelInstitute of Physiology I, Life and Brain Center, University of Bonn, 53105 Bonn, Germany.
Katrin M BüllesbachMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Tobias BaldDepartment of Dermatology and Allergy, Laboratory of Experimental Dermatology, University of Bonn, 53105 Bonn, Germany.
Asuka InoueGraduate School of Pharmaceutical Sciences, Tohoku University, 6-3, Aoba, Aramaki, Aoba-ku, Sendai City 980-0065, Japan.
Yuji ShinjoGraduate School of Pharmaceutical Sciences, Tohoku University, 6-3, Aoba, Aramaki, Aoba-ku, Sendai City 980-0065, Japan.
Ségolène GalandrinInstitut des Maladies Métaboliques et Cardiovasculaires, Institut Nataional de la Santé et de la Recherche Médicale, Université Toulouse III Paul Sabatier, 31432 Toulouse, France.
Naveen ShridharDepartment of Dermatology and Allergy, Laboratory of Experimental Dermatology, University of Bonn, 53105 Bonn, Germany.
Michael HesseInstitute of Physiology I, Life and Brain Center, University of Bonn, 53105 Bonn, Germany.
Manuel GrundmannMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Nicole MertenMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Thomas H CharpentierDepartment of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina 27599, USA.
Matthew MartzDepartment of Biochemistry and Biophysics, University of North Carolina School of Medicine, Chapel Hill, North Carolina 27599, USA.
Adrian J ButcherMedical Research Council Toxicology Unit, University of Leicester, Hodgkin building, Leicester LE1 9HN, UK.
Tanja SlodczykDepartment of Dermatology and Allergy, Laboratory of Experimental Dermatology, University of Bonn, 53105 Bonn, Germany.
Sylvain ArmandoDepartment of Medicine, McGill University, and the Research Institute of the McGill University Health Centre, Montreal, Quebec, Canada H4A 3J1.
Maike EffernDepartment of Clinical Chemistry and Clinical Pharmacology, University of Bonn, 53105 Bonn, Germany.
Yoon NamkungDepartment of Medicine, McGill University, and the Research Institute of the McGill University Health Centre, Montreal, Quebec, Canada H4A 3J1.
Laura JenkinsMolecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, Scotland G12 8QQ, UK.
Velten HornEduard-Zintl-Institute of Inorganic and Physical Chemistry, Technische Universität Darmstadt, 64287 Darmstadt, Germany.
Anne StößelPharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, 53121 Bonn, Germany.
Harald DargatzMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Daniel TietzeEduard-Zintl-Institute of Inorganic and Physical Chemistry, Technische Universität Darmstadt, 64287 Darmstadt, Germany.
Diana ImhofPharmaceutical Chemistry I, Institute of Pharmacy, University of Bonn, 53121 Bonn, Germany.
Céline GalésInstitut des Maladies Métaboliques et Cardiovasculaires, Institut Nataional de la Santé et de la Recherche Médicale, Université Toulouse III Paul Sabatier, 31432 Toulouse, France.
Christel DrewkeMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Christa E MüllerPharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, 53121 Bonn, Germany.
Michael HölzelDepartment of Clinical Chemistry and Clinical Pharmacology, University of Bonn, 53105 Bonn, Germany.
Graeme MilliganMolecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, Scotland G12 8QQ, UK.
Andrew B TobinMedical Research Council Toxicology Unit, University of Leicester, Hodgkin building, Leicester LE1 9HN, UK.
Jesús GomezaMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Henrik G DohlmanDepartment of Biochemistry and Biophysics, University of North Carolina School of Medicine, Chapel Hill, North Carolina 27599, USA.
John SondekDepartment of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina 27599, USA.
T Kendall HardenDepartment of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina 27599, USA.
Michel BouvierDepartment of Biochemistry and Institute for Research in Immunology and Cancer, Université de Montréal, Montreal, Québec, Canada QC H3C IJ4.ORCID http://orcid.org/0000-0003-1128-0100
Stéphane A LaporteDepartment of Medicine, McGill University, and the Research Institute of the McGill University Health Centre, Montreal, Quebec, Canada H4A 3J1.
Junken AokiGraduate School of Pharmaceutical Sciences, Tohoku University, 6-3, Aoba, Aramaki, Aoba-ku, Sendai City 980-0065, Japan.
Bernd K FleischmannInstitute of Physiology I, Life and Brain Center, University of Bonn, 53105 Bonn, Germany.
Klaus MohrPharmacology &Toxicology Section, Institute of Pharmacy, University of Bonn, 53121 Bonn, Germany.
Gabriele M KönigInstitute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Thomas TütingDepartment of Dermatology and Allergy, Laboratory of Experimental Dermatology, University of Bonn, 53105 Bonn, Germany.
Evi KostenisMolecular, Cellular and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
University of Bonn · DEUniversity of North Carolina at Chapel Hill · USMcGill University Health Centre · CATohoku University · JPTechnische Universität Darmstadt · DEUniversité Toulouse III - Paul Sabatier · FRUniversity of Glasgow · GBUniversity of Leicester · GBInstitute for Research in Immunology and Cancer · CA
Funding
Virology Research Program (Program 4)P30CA016086 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI Deborah F. Tate · 1985 to 2026
$201.5MIntegrated Training in Cancer Model SystemsT32CA009156 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI DER, CHANNING J. · 1985 to 2020
$19.7MRegulation of Phospholipase CR01GM057391 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI SONDEK, JOHN E · 1998 to 2021
$6.9MNegative and positive feedback in cell signalingR35GM118105 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI Henrik G. Dohlman · 2016 to 2026
$6.6MREGULATORS OF G PROTEIN SIGNALING IN YEASTR01GM059167 · NIGMS · YALE UNIVERSITY · PI DOHLMAN, HENRIK G. · 1999 to 2015
$3.7MBiotechnology and Biological Sciences Research Council BB/K019864/1Medical Research Council MC_UP_A600_1110NCI NIH HHS P30 CA016086NCI NIH HHS T32 CA009156NCI NIH HHS T32 CA009156-40NIGMS NIH HHS R01 GM057391NIGMS NIH HHS R01 GM059167NIGMS NIH HHS R35 GM118105
Abstract
Despite the discovery of heterotrimeric αβγ G proteins ∼25 years ago, their selective perturbation by cell-permeable inhibitors remains a fundamental challenge. Here we report that the plant-derived depsipeptide FR900359 (FR) is ideally suited to this task. Using a multifaceted approach we systematically characterize FR as a selective inhibitor of Gq/11/14 over all other mammalian Gα isoforms and elaborate its molecular mechanism of action. We also use FR to investigate whether inhibition of Gq proteins is an effective post-receptor strategy to target oncogenic signalling, using melanoma as a model system. FR suppresses many of the hallmark features that are central to the malignancy of melanoma cells, thereby providing new opportunities for therapeutic intervention. Just as pertussis toxin is used extensively to probe and inhibit the signalling of Gi/o proteins, we anticipate that FR will at least be its equivalent for investigating the biological relevance of Gq.
Indexed as
AnimalsArdisiaCell Line, TumorDepsipeptidesGene Expression Regulation, NeoplasticGTP-Binding Protein alpha Subunits, Gq-G11HumansMelanomaMiceModels, MolecularMolecular StructureProtein ConformationProtein IsoformsSignal TransductionTailVasoconstrictionDepsipeptidesFR900359GTP-Binding Protein alpha Subunits, Gq-G11Protein Isoforms
Identifiers
What OpenQuestion holds
Textmetadata
LicenceCC BY
Read underepoch 390
Registered trials
None linked
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.