ArticleJournal of medicinal chemistry2020
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity
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Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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17 citing papers in PubMed, 26 citations in OpenAlex.
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- CAMK1D activates AMPK/PINK1/Parkin-dependent mitophagy to promote enzalutamide resistance in prostate cancer.Cell death & disease · 2025Article
- Integrated Genomic-Metabolomic Analysis for Tri-Categorical Classification of Type 2 Diabetes Status in the Korean Ansan-Ansung Cohort.International journal of molecular sciences · 2025Article
- CAMKK1 in Obesity and Type 2 Diabetes Mellitus: Evidence of Interaction With Appetite-Regulating, Metabolic and Inflammatory Factors.Endocrinology, diabetes & metabolism · 2025Article
- Single-Step Genome-Wide Association Study of Factors for Evaluated and Linearly Scored Traits in Swedish Warmblood Horses.Journal of animal breeding and genetics = Zeitschrift fur Tierzuchtung und Zuchtungsbiologie · 2025Article
- The role of metal ion metabolism in the pathogenesis of diabetes and associated complications.Frontiers in endocrinology · 2025Review
- Podocyte-specific KLF6 primes proximal tubule CaMK1D signaling to attenuate diabetic kidney disease.Nature communications · 2024Article
- Synthesis of chiral sulfilimines by organocatalytic enantioselective sulfur alkylation of sulfenamides.Science advances · 2024Article
- Comprehensive analysis of key host gene-microbe networks in the cecum tissues of the obese rabbits induced by a high-fat diet.Frontiers in cellular and infection microbiology · 2024Article
- Epigenome-wide DNA methylation analysis of myasthenia gravis.FEBS open bio · 2023Article
- AI-Assisted chemical probe discovery for the understudied Calcium-Calmodulin Dependent Kinase, PNCK.PLoS computational biology · 2023Article
- Integrated Bioinformatics Analysis Identifies Robust Biomarkers and Its Correlation With Immune Microenvironment in Nonalcoholic Fatty Liver Disease.Frontiers in genetics · 2022Article
- Effects of Specific Inhibitors for CaMK1D on a Primary Neuron Model for Alzheimer's Disease.Molecules (Basel, Switzerland) · 2021Article
- Genetic Variants in Transcription Factor Binding Sites in Humans: Triggered by Natural Selection and Triggers of Diseases.International journal of molecular sciences · 2021Review
- Backbone resonance assignments of the catalytic and regulatory domains of CaBiomolecular NMR assignments · 2020Article
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Authors and funding
34 authors at 12 institutions in 5 countries.
Christophe FromontCentre for Biomolecular Sciences and School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, U.K.
Alessio AtzoriCentre for Biomolecular Sciences and School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, U.K.
Divneet KaurCentre for Biomolecular Sciences and School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, U.K.
Lubna HashmiCentre for Biomolecular Sciences and School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, U.K.
Graziella GrecoSchool of Pharmacy, College of Medical and Dental Sciences, University of Birmingham, Edgbaston B15 2TT, U.K.
Alejandro CabanillasSchool of Pharmacy, College of Medical and Dental Sciences, University of Birmingham, Edgbaston B15 2TT, U.K.
Huy Van NguyenSchool of Pharmacy, College of Medical and Dental Sciences, University of Birmingham, Edgbaston B15 2TT, U.K.ORCID 0000-0002-3985-1510
D Heulyn JonesDivision of Pharmacy and Optometry, School of Health Sciences, Manchester Academic Health Sciences Centre, University of Manchester, Manchester M13 9PL, U.K.
Miguel GarzónDivision of Pharmacy and Optometry, School of Health Sciences, Manchester Academic Health Sciences Centre, University of Manchester, Manchester M13 9PL, U.K.
Ana VarelaDivision of Pharmacy and Optometry, School of Health Sciences, Manchester Academic Health Sciences Centre, University of Manchester, Manchester M13 9PL, U.K.
Brett StevensonSygnature Discovery, BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K.
Greg P IacobiniSygnature Discovery, BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K.
Marc LenoirInstitute of Cancer and Genomic Sciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, U.K.
Sundaresan RajeshInstitute of Cancer and Genomic Sciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, U.K.
Clare BoxInstitute of Cancer and Genomic Sciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, U.K.
Jitendra KumarDepartment of Biochemistry, University of Alberta, Edmonton, Alberta T6G 2H7, Canada.
Paige GrantDepartment of Biochemistry, University of Alberta, Edmonton, Alberta T6G 2H7, Canada.
Vera NovitskayaInstitute of Cancer and Genomic Sciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, U.K.
Juliet MorganSygnature Discovery, BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K.
Fiona J SorrellStructural Genomics Consortium and Target Discovery Institute, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford OX3 7DQ, U.K.
Clara RedondoStructural Genomics Consortium and Target Discovery Institute, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford OX3 7DQ, U.K.
Andreas KramerStructural Genomics Consortium and Buchmann Institute for Molecular Life Sciences, Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Straße 9, 60438 Frankfurt am Main, Germany.
C John HarrisCJH Consultants, Ford Cottage, South Weirs, Burley Road, Brockenhurst, Hants SO42 7UQ, U.K.
Brendan LeightonThe Research Network, IPC 600 Discovery Park, Ramsgate Road, Sandwich CT13 9NJ, U.K.
Steven P VickersRenaSci Limited, BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K.
Sharon C CheethamRenaSci Limited, BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K.
Colin KenyonDST/NRF Centre of Excellence for Biomedical Tuberculosis Research, SAMRC Centre for Molecular and Cellular Biology, Division of Molecular Biology and Human Genetics, Faculty of Medicine and Health Sciences, Stellenbosch University, Cape Town 8000, South Africa.
Anna M GrabowskaEx Vivo Cancer Pharmacology Centre of Excellence, Cancer Biology, Division of Cancer and Stem Cells, School of Medicine, University of Nottingham, Nottingham NG7 2RD, U.K.
Michael OverduinDepartment of Biochemistry, University of Alberta, Edmonton, Alberta T6G 2H7, Canada.
Fedor BerditchevskiInstitute of Cancer and Genomic Sciences, University of Birmingham, Edgbaston, Birmingham B15 2TT, U.K.
Chris J WestonCentre for Liver Research, Institute of Immunology and Immunotherapy, University of Birmingham, Birmingham, B15 2TT, U.K.
Stefan KnappStructural Genomics Consortium and Buchmann Institute for Molecular Life Sciences, Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Straße 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0001-5995-6494
Peter M FischerCentre for Biomolecular Sciences and School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, U.K.ORCID 0000-0002-5866-9271
Sam ButterworthDivision of Pharmacy and Optometry, School of Health Sciences, Manchester Academic Health Sciences Centre, University of Manchester, Manchester M13 9PL, U.K.ORCID 0000-0002-6549-3753
University of Birmingham · GBUniversity of Nottingham · GBManchester Academic Health Science Centre · GBSignature Research (United States) · USUniversity of Alberta · CAGenomics England · GBGoethe University Frankfurt · DERenaSci (United Kingdom) · GBBrockenhurst College · GBNIHR Birmingham Liver Biomedical Research Unit · GBPfizer (United Kingdom) · GBSouth African Medical Research Council · ZA
Funding
Medical Research Council MC_PC_15032Wellcome Trust 103022Wellcome Trust 202708Wellcome Trust MC_PC_15032
Abstract
Polymorphisms in the region of the calmodulin-dependent kinase isoform D (CaMK1D) gene are associated with increased incidence of diabetes, with the most common polymorphism resulting in increased recognition by transcription factors and increased protein expression. While reducing CaMK1D expression has a potentially beneficial effect on glucose processing in human hepatocytes, there are no known selective inhibitors of CaMK1 kinases that can be used to validate or translate these findings. Here we describe the development of a series of potent, selective, and drug-like CaMK1 inhibitors that are able to provide significant free target cover in mouse models and are therefore useful as
Indexed as
Drug DiscoveryInsulin ResistanceAnimalsCalcium-Calmodulin-Dependent Protein Kinase Type 1DietDisease Models, AnimalMaleMiceMice, Inbred C57BLModels, MolecularObesityProtein ConformationProtein Kinase InhibitorsCalcium-Calmodulin-Dependent Protein Kinase Type 1Camk1d protein, mouseProtein Kinase Inhibitors
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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.