ArticleNature communications2015
A RIPK2 inhibitor delays NOD signalling events yet prevents inflammatory cytokine production.
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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 73 papers.
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73citing papers in PubMed
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73 citing papers in PubMed.
- A Nelore Cattle Structural Variant Catalog.Animal genetics · 2026Article
- Peptidoglycan Suppresses Melanoma Growth in a Murine Model with Local Immune Activation.International journal of molecular sciences · 2026Article
- Identification of Cellular Senescence-Related Hub Genes in Rheumatoid Arthritis from Bioinformatics Analysis Through Machine Learning up to Verifications in Mouse Macrophages and Tests in Patients.International journal of molecular sciences · 2026Article
- The dual role of RIPK family in IBD: from cell death to therapeutic targeting.Molecular medicine (Cambridge, Mass.) · 2026Review
- Escherichia coli promotes colorectal cancer metastasis by maintaining enhancer-promoter loops through releasing neutrophil extracellular traps.Nature communications · 2026Article
- RNA stability: a novel perspective on gene regulatory networks in bovine mastitis.BMC genomics · 2025Article
- Distinct colitis-associated macrophages drive NOD2-dependent bacterial sensing and gut homeostasis.The Journal of clinical investigation · 2025Article
- NLRP3 inflammasome-driven hemophagocytic lymphohistiocytosis occurs independent of IL-1β and IL-18 and is targetable by BET inhibitors.Science advances · 2025Article
- CMD-OPT model enables the discovery of a potent and selective RIPK2 inhibitor as preclinical candidate for the treatment of acute liver injury.Acta pharmaceutica Sinica. B · 2025Article
- A transformer-based strategy to develop RP20 as a potent RIPK2 inhibitor for acetaminophen-induced acute liver injury.Acta pharmaceutica Sinica. B · 2025Article
- Article
- MYSM1 attenuates osteoarthritis by recruiting PP2A to deubiquitinate and dephosphorylate RIPK2.Bone research · 2025Article
- Current advances on RIPK2 and its inhibitors in pathological processes: a comprehensive review.Frontiers in molecular neuroscience · 2025Review
- Ripks and Neuroinflammation.Molecular neurobiology · 2024Review
- Pharmacological inhibition of receptor-interacting protein kinase 2 (RIPK2) elicits neuroprotective effects following experimental ischemic stroke.Experimental neurology · 2024Article
- Mettl3‑mediated mMolecular medicine reports · 2024Article
- Receptor-interacting protein kinase 2 is associated with tumor immune infiltration, immunotherapy-related biomarkers, and affects gastric cancer cells growthJournal of Cancer · 2024Article
- Design, synthesis and biological evaluation of 4-aminoquinoline derivatives as receptor-interacting protein kinase 2 (RIPK2) inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- OTUD1 ameliorates cerebral ischemic injury through inhibiting inflammation by disrupting K63-linked deubiquitination of RIP2.Journal of neuroinflammation · 2023Article
- Structure shows that the BIR2 domain of E3 ligase XIAP binds across the RIPK2 kinase dimer interface.Life science alliance · 2023Article
13 more citing papers are in PubMed but not listed here.
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Authors and funding
28 authors.
Ueli Nachbur1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Che A Stafford1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Aleksandra Bankovacki1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Yifan Zhan1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Lisa M Lindqvist1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Berthe K Fiil1] Department of Disease Biology, Novo Nordisk Foundation Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark [2] Ludwig Institute for Cancer Research, Nuffield Department of Clinical Medicine, University of Oxford, Oxford OX3 7DQ, UK.
Yelena Khakham1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Hyun-Ja Ko1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Jarrod J Sandow1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Hendrik Falk1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia [3] Cancer Therapeutics CRC, Bundoora, Victoria 3083, Australia.
Jessica K HolienACRF Rational Drug Discovery Centre, St Vincent's Institute of Medical Research, 9 Princes Street, Fitzroy, Victoria 3065, Australia.ORCID 0000000287352871
Diep Chau1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Joanne Hildebrand1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
James E Vince1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Phillip P Sharp1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Andrew I Webb1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Katherine A JackmanThe Florey Institute of Neuroscience and Mental Health, Melbourne Brain Centre, Austin Campus, 245 Burgundy Street, Heidelberg, Victoria 3084, Australia.
Sabrina MühlenDepartment of Microbiology and Immunology, University of Melbourne, Victoria 3010, Australia.
Catherine L KennedyDepartment of Microbiology and Immunology, University of Melbourne, Victoria 3010, Australia.
Kym N Lowes1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
James M Murphy1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Mads Gyrd-Hansen1] Department of Disease Biology, Novo Nordisk Foundation Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark [2] Ludwig Institute for Cancer Research, Nuffield Department of Clinical Medicine, University of Oxford, Oxford OX3 7DQ, UK.
Michael W Parker1] ACRF Rational Drug Discovery Centre, St Vincent's Institute of Medical Research, 9 Princes Street, Fitzroy, Victoria 3065, Australia [2] Department of Biochemistry and Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, Parkville, Victoria 3010, Australia.ORCID 0000000231011138
Elizabeth L HartlandDepartment of Microbiology and Immunology, University of Melbourne, Victoria 3010, Australia.
Andrew M Lew1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
David C S Huang1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
Guillaume Lessene1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.
John Silke1] The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia [2] Department of Medical Biology, University of Melbourne, Melbourne, Victoria 3010, Australia.ORCID 0000000276115774
Funding
No grant is acknowledged in the PubMed record.
Abstract
Intracellular nucleotide binding and oligomerization domain (NOD) receptors recognize antigens including bacterial peptidoglycans and initiate immune responses by triggering the production of pro-inflammatory cytokines through activating NF-κB and MAP kinases. Receptor interacting protein kinase 2 (RIPK2) is critical for NOD-mediated NF-κB activation and cytokine production. Here we develop and characterize a selective RIPK2 kinase inhibitor, WEHI-345, which delays RIPK2 ubiquitylation and NF-κB activation downstream of NOD engagement. Despite only delaying NF-κB activation on NOD stimulation, WEHI-345 prevents cytokine production in vitro and in vivo and ameliorates experimental autoimmune encephalomyelitis in mice. Our study highlights the importance of the kinase activity of RIPK2 for proper immune responses and demonstrates the therapeutic potential of inhibiting RIPK2 in NOD-driven inflammatory diseases.
Indexed as
Adenosine TriphosphateAnimalsChromatography, LiquidCytokinesEncephalomyelitis, Autoimmune, ExperimentalFemaleHumansImmune SystemInflammationInhibitory Concentration 50Interferon-gammaMaleMAP Kinase Signaling SystemMiceMice, Inbred C57BLMice, Inbred NODAdenosine TriphosphateCytokinesInterferon-gammaNF-kappa BReceptor-Interacting Protein Serine-Threonine Kinase 2Receptor-Interacting Protein Serine-Threonine KinasesRecombinant ProteinsRIPK2 protein, humanRipk2 protein, mouseUbiquitin
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PMID
25778803What OpenQuestion holds
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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.