ArticleNeuropharmacology2023
Characterisation of C101248: A novel selective THIK-1 channel inhibitor for the modulation of microglial NLRP3-inflammasome.
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Article in Neuropharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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15citing papers in PubMed
2.2field-weighted citation impact, top 12% of its field
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Who cites it
15 citing papers in PubMed, 28 citations in OpenAlex.
- The axon initial segment-associated microglia regulate neuronal activity and visual perception.Cell research · 2026Article
- THIK-1 channel mediates microglial glucose sensing and modulates AgRP neurons.bioRxiv : the preprint server for biology · 2026Article
- Inhibitory effect of 17β-estradiol on the THIK-1 channel.PloS one · 2026Article
- Pro-inflammatory diet mediates the association between epilepsy and sleep disorders: A cross-sectional study.Ibrain · 2026Article
- The chloride intracellular channel 1 (CLIC1) is essential for microglial morphodynamics and neuroinflammation.Science advances · 2025Article
- Structure of the human KNature structural & molecular biology · 2025Article
- Cryo-EM structure of the human THIK-1 K2P KNature structural & molecular biology · 2025Article
- The cryo-EM structure and physical basis for anesthetic inhibition of the THIK1 K2P channel.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- NETSseq reveals inflammatory and aging mechanisms in distinct cell types, driving cerebellar decline in ataxia telangiectasia.Frontiers in neuroscience · 2025Article
- Structure of the human KbioRxiv : the preprint server for biology · 2024Article
- Discovery of CVN293, a Brain Permeable KCNK13 (THIK-1) Inhibitor Suitable for Clinical Assessment.ACS medicinal chemistry letters · 2024Article
- Differential contribution of THIK-1 KJournal of neuroinflammation · 2024Article
- Modulation of Microglial Function by ATP-Gated P2X7 Receptors: Studies in Rat, Mice and Human.Cells · 2024Review
- Research progress of two-pore potassium channel in myocardial ischemia-reperfusion injury.Frontiers in physiology · 2024Review
- Unlocking the therapeutic potential of P2X7 receptor: a comprehensive review of its role in neurodegenerative disorders.Frontiers in pharmacology · 2024Review
Corrections and comments
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Authors and funding
31 authors at 5 institutions in 2 countries.
Bernardino OssolaCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK. Electronic address: dino.ossola@cerevance.com.
Ali RifatCharité - Universitätsmedizin Berlin, corporate member of Freie Universität Berlin and Humboldt-Universität zu Berlin, Institute of Neurophysiology, Charitéplatz 1, 10117 Berlin, Germany; Berlin Institute of Health at Charité - Universitätsmedizin Berlin, Charitéplatz 1, 10117, Berlin, Germany.
Anna RowlandCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Helen HunterCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Samuel DrinkallBerlin Institute of Health at Charité - Universitätsmedizin Berlin, Charitéplatz 1, 10117, Berlin, Germany.
Clare BenderCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Mayida HamlischerCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Martin TeallCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Russell BurleyCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Daneil F BarkerCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
David CadwalladrCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Louise DicksonCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Jason M K LawrenceCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Jenna R M HarveyCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Marina LizioCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Xiao XuCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Edel KavanaghCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Toni CheungCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Steve SheardownCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Catherine B LawrenceDivision of Neuroscience and Experimental Psychology, School of Biological Sciences, Faculty of Biology, Medicine and Health, University of Manchester, Manchester Academic Health Science Centre, Manchester, UK; Geoffrey Jefferson Brain Research Centre, The Manchester Academic Health Science Centre, Northern Care Alliance NHS Group, University of Manchester, Manchester, UK; The Lydia Becker Institute of Immunology and Inflammation, University of Manchester, Manchester, UK.
Michael HarteDivision of Pharmacy & Optometry, School of Health Sciences, Faculty of Biology, Medicine and Health, University of Manchester, Manchester Academic Health Science Centre, Manchester, UK; The Lydia Becker Institute of Immunology and Inflammation, University of Manchester, Manchester, UK.
David BroughDivision of Neuroscience and Experimental Psychology, School of Biological Sciences, Faculty of Biology, Medicine and Health, University of Manchester, Manchester Academic Health Science Centre, Manchester, UK; Geoffrey Jefferson Brain Research Centre, The Manchester Academic Health Science Centre, Northern Care Alliance NHS Group, University of Manchester, Manchester, UK; The Lydia Becker Institute of Immunology and Inflammation, University of Manchester, Manchester, UK.
Christian MadryCharité - Universitätsmedizin Berlin, corporate member of Freie Universität Berlin and Humboldt-Universität zu Berlin, Institute of Neurophysiology, Charitéplatz 1, 10117 Berlin, Germany.
Kim MatthewsCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Kevin DoyleCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Keith PageCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Justin PowellCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Nicola L BriceCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Roland W BürliCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Mark B CarltonCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Lee A DawsonCerevance Ltd, 418 Cambridge Science Park, Milton Road, Cambridge, CB4 0PZ, UK.
Covance (United Kingdom) · GBManchester Academic Health Science Centre · GBHumboldt-Universität zu Berlin · DEBerlin Institute of Health at Charité - Universitätsmedizin Berlin · DECambridge Environmental Research Consultants (United Kingdom) · GB
Funding
Medical Research Council MR/T016515/1
Abstract
Neuroinflammation, specifically the NLRP3 inflammasome cascade, is a common underlying pathological feature of many neurodegenerative diseases. Evidence suggests that NLRP3 activation involves changes in intracellular K
Indexed as
Alzheimer DiseaseInflammasomesPotassium Channels, Tandem Pore DomainAnimalsBrainHumansMiceMicrogliaNeuroinflammatory DiseasesNLR Family, Pyrin Domain-Containing 3 ProteinInflammasomesKCNK13 protein, humanKcnk13 protein, mouseNLR Family, Pyrin Domain-Containing 3 ProteinNlrp3 protein, mousePotassium Channels, Tandem Pore DomainAlzheimer's diseaseKCNK13MicrogliaNeuroinflammationNLRP3 inflammasomeTHIK-1
Identifiers
What OpenQuestion holds
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LicenceCC BY
Read underepoch 390
Registered trials
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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.