ArticleCell2017
Artemisinins Target GABA
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Article in Cell, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 191 papers, 1 of them a synthesis that pooled it.
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191citing papers in PubMed, 1 pooled it
47.7field-weighted citation impact, top 1% of its field
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Who cites it
191 citing papers in PubMed, 1 synthesis or guideline pooled it, 373 citations in OpenAlex.
- Protective Effect and Possible Mechanisms of Artemisinin and Its Derivatives for Diabetic Nephropathy: A Systematic Review and Meta-Analysis in Animal Models.Oxidative medicine and cellular longevity · 2022Pooled it
- Long-term gamma-aminobutyric acid (GABA) treatment fails to regain beta-cell function in longstanding type 1 diabetes in a randomized trial.Scientific reports · 2025Trial
- Direct ultrastructural validation of endocrine cell identity in zebrafish pancreatic islets.Cell and tissue research · 2026Article
- Metabolic reprogramming drives pancreatic β cell neogenesis from α cells.Nature chemical biology · 2026Article
- Synaptic vs. Non-Synaptic Glycine Receptors: Physiological Role and Implications in Alzheimer's Disease Pathology.International journal of molecular sciences · 2026Review
- Resolving human α versus β cell fate allocation for the generation of stem cell-derived islets.Nature communications · 2026Article
- Recent advances in proteomic strategies for target identification of traditional Chinese medicine.Journal of pharmaceutical analysis · 2026Review
- Abnormally Elevated PKCδ Delays Diabetic Wound Healing by Inhibiting the GAD1-GABA Pathway.Diabetes & metabolism journal · 2026Article
- Artemisinin derivative SM934 targets α-enolase to inhibit PEP-mediated TAK1 stabilization and inflammation.Science China. Life sciences · 2026Article
- The Role of Microbiota in Type 1 Diabetes: Insights into Dysbiosis and Immune Interactions.Nutrients · 2026Review
- Progress and application of activity-based protein profiling for the discovery of natural product targets.Molecular diversity · 2026Review
- Heme as activator and target for artemisinin: Towards multiple pharmacological bioactivity.Biochemistry and biophysics reports · 2026Review
- Mosloflavone induces pancreatic α cells transdifferentiation into β cells through PDX1.Journal of natural medicines · 2026Article
- Benchmarking porcine pancreatic ductal organoids for drug screening applications.EMBO molecular medicine · 2025Article
- The contrasting effects of two antimalarial drugs on insulin secretion.Cellular and molecular life sciences : CMLS · 2025Article
- Drug-induced regeneration of pancreatic beta cells: An approach to cellular therapeutic targets.Cell regeneration (London, England) · 2025Review
- Review
- Is the Activation of the Postsynaptic Ligand Gated Glycine- or GABABiomedicines · 2025Review
- Target identification of natural products in cancer with chemical proteomics and artificial intelligence approaches.Cancer biology & medicine · 2025Review
- Article
131 more citing papers are in PubMed but not listed here.
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Authors and funding
40 authors at 12 institutions in 7 countries.
Jin LiCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Tamara CasteelsCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Thomas FrogneNovo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark.
Camilla IngvorsenNovo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark.
Christian HonoréNovo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark.
Monica CourtneyUniversité Côte d'Azur, INSERM, CNRS, iBV, 06108 Nice, France.
Kilian V M HuberCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Nicole SchmitnerInstitute of Molecular Biology, Leopold-Franzens-University Innsbruck, Technikerstr. 25, 6020 Innsbruck, Austria.
Robin A KimmelInstitute of Molecular Biology, Leopold-Franzens-University Innsbruck, Technikerstr. 25, 6020 Innsbruck, Austria.
Roman A RomanovDepartment of Molecular Neurosciences, Center for Brain Research, Medical University of Vienna, 1090 Vienna, Austria; Department of Neuroscience, Karolinska Institutet, 171 77 Stockholm, Sweden.
Caterina SturtzelChildren's Cancer Research Institute, Innovative Cancer Models, Zimmermannplatz 10, 1090 Vienna, Austria.
Charles-Hugues LardeauCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria; Christian Doppler Laboratory for Chemical Epigenetics and Antiinfectives, CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, Lazarettgasse 14, 1090 Vienna, Austria.
Johanna KlughammerCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Matthias FarlikCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Sara SdelciCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Andhira VieiraUniversité Côte d'Azur, INSERM, CNRS, iBV, 06108 Nice, France.
Fabio AvolioUniversité Côte d'Azur, INSERM, CNRS, iBV, 06108 Nice, France.
François BriandPhysiogenex S.A.S., Prologue Biotech, 516, rue Pierre et Marie Curie, 31670 Labege, France.
Igor BaburinInstitute of Pharmacology and Toxicology, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria.
Peter MájekCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Florian M PaulerCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Thomas PenzCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Alexey StukalovCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Manuela GridlingCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Katja ParapaticsCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Charlotte BarbieuxCell Isolation and Transplantation Center, Department of Surgery, Geneva University Hospitals and University of Geneva, 1211 Geneva, Switzerland.
Ekaterine BerishviliCell Isolation and Transplantation Center, Department of Surgery, Geneva University Hospitals and University of Geneva, 1211 Geneva, Switzerland; Institute of Medical Research, Ilia State University, Tbilisi 0162, Georgia.
Andreas SpittlerCore Facility Flow Cytometry and Department of Surgery, Research Laboratories, Medical University of Vienna, 1090 Vienna, Austria.
Jacques ColingeCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Keiryn L BennettCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria.
Steffen HeringInstitute of Pharmacology and Toxicology, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria.
Thierry SulpicePhysiogenex S.A.S., Prologue Biotech, 516, rue Pierre et Marie Curie, 31670 Labege, France.
Christoph BockCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria; Department of Laboratory Medicine, Medical University of Vienna, 1090 Vienna, Austria; Max Planck Institute for Informatics, 66123 Saarbrücken, Germany.
Martin DistelChildren's Cancer Research Institute, Innovative Cancer Models, Zimmermannplatz 10, 1090 Vienna, Austria.
Tibor HarkanyDepartment of Molecular Neurosciences, Center for Brain Research, Medical University of Vienna, 1090 Vienna, Austria; Department of Neuroscience, Karolinska Institutet, 171 77 Stockholm, Sweden.
Dirk MeyerInstitute of Molecular Biology, Leopold-Franzens-University Innsbruck, Technikerstr. 25, 6020 Innsbruck, Austria.
Giulio Superti-FurgaCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria; Center for Physiology and Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
Patrick CollombatUniversité Côte d'Azur, INSERM, CNRS, iBV, 06108 Nice, France.
Jacob Hecksher-SørensenNovo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark.
Stefan KubicekCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences. Lazarettgasse 14, 1090 Vienna, Austria; Christian Doppler Laboratory for Chemical Epigenetics and Antiinfectives, CeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, Lazarettgasse 14, 1090 Vienna, Austria. Electronic address: skubicek@cemm.oeaw.ac.at.
Austrian Academy of Sciences · ATNovo Nordisk (Denmark) · DKMedical University of Vienna · ATUniversität Innsbruck · ATInserm · FRPhysiogenex (France) · FRUniversité Côte d'Azur · FRUniversity of Vienna · ATCeMM Research Center for Molecular Medicine · ATKarolinska Institutet · SEUniversity Hospital of Geneva · CHUniversity of Geneva · CH
Funding
The Human Islet Distribution Coordinating Center (UC4)UC4DK098085 · NIDDK · BECKMAN RESEARCH INSTITUTE/CITY OF HOPE · PI EVANS-MOLINA, CARMELLA, NILAND, JOYCE CAROL · 2012 to 2017
$25.6MNIDDK NIH HHS UC4 DK098085
Abstract
Type 1 diabetes is characterized by the destruction of pancreatic β cells, and generating new insulin-producing cells from other cell types is a major aim of regenerative medicine. One promising approach is transdifferentiation of developmentally related pancreatic cell types, including glucagon-producing α cells. In a genetic model, loss of the master regulatory transcription factor Arx is sufficient to induce the conversion of α cells to functional β-like cells. Here, we identify artemisinins as small molecules that functionally repress Arx by causing its translocation to the cytoplasm. We show that the protein gephyrin is the mammalian target of these antimalarial drugs and that the mechanism of action of these molecules depends on the enhancement of GABA
Indexed as
Disease Models, AnimalSignal TransductionAnimalsArtemetherArtemisininsCarrier ProteinsCells, CulturedCell TransdifferentiationDiabetes MellitusDiabetes Mellitus, Type 1gamma-Aminobutyric AcidGene Expression ProfilingHomeodomain ProteinsHumansInsulinIslets of LangerhansArtemetherArtemisininsARX protein, humanCarrier Proteinsgamma-Aminobutyric AcidgephyrinHomeodomain ProteinsInsulinMembrane ProteinsReceptors, GABA-ATranscription FactorsartemisininsARX translocationchemical biologydiabetesGABA-receptor signalinggephyrininsulin secretionpancreatic endocrine transdifferentiationregenerative medicineβ cell
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LicenceCC BY-NC-ND
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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.