ArticleJournal of medicinal chemistry2021
New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
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Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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21citing papers in PubMed
1.5field-weighted citation impact, top 17% of its field
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Who cites it
21 citing papers in PubMed, 31 citations in OpenAlex.
- Eyes Toward the Clinic: Selective Inhibition and Degradation Approaches to Bromodomain-Containing Proteins.Chembiochem : a European journal of chemical biology · 2026Review
- Development of a Lysine-Reactive Targeted Covalent Inhibitor for the P300/CBP-Associated Factor Bromodomain Through Structure-Based Design.ChemMedChem · 2026Article
- An epigenetic bifunctional that toggles between transactivation and repression.bioRxiv : the preprint server for biology · 2026Article
- NanoBRET Tracer Development for Class I Bromodomain Target Engagement in Live Cells.Bioconjugate chemistry · 2026Article
- Role of Spatial Heterogeneity in Muscle-Invasive Bladder Cancer on Overall Survival and Immunotherapy Response.Cancers · 2026Article
- NanoBRET Tracer Development for Class I Bromodomain Target Engagement in Live Cells.bioRxiv : the preprint server for biology · 2025Article
- BPTF-665aa mediate chromatin remodeling drives chemoresistance in T-LBL/ALL.Journal of experimental & clinical cancer research : CR · 2025Article
- Loss of BPTF restores estrogen response and suppresses metastasis of mammary tumors.Nature communications · 2025Article
- BPTF Target Engagement by Acetylated H2A.Z Photoaffinity Probes.Biochemistry · 2025Article
- KAT6A chimeras form a self-reinforcing epigenetic module with NURF and MLL/COMPASS to sustain AML.Genome biology · 2025Article
- A BPTF-specific PROTAC degrader enhances NK cell-based cancer immunotherapy.Molecular therapy : the journal of the American Society of Gene Therapy · 2025Article
- Chromatin remodellers as therapeutic targets.Nature reviews. Drug discovery · 2024Review
- lncRNA LINC00941 modulates MTA2/NuRD occupancy to suppress premature human epidermal differentiation.Life science alliance · 2024Article
- Context-specific functions of chromatin remodellers in development and disease.Nature reviews. Genetics · 2024Review
- Article
- Bromodomain inhibitors and therapeutic applications.Current opinion in chemical biology · 2023Review
- Design of Class I/IV Bromodomain-Targeting Degraders for Chromatin Remodeling Complexes.ACS chemical biology · 2023Article
- BAP18 facilitates CTCF-mediated chromatin accessible to regulate enhancer activity in breast cancer.Cell death and differentiation · 2023Article
- Targeting Chromatin-Remodeling Factors in Cancer Cells: Promising Molecules in Cancer Therapy.International journal of molecular sciences · 2022Review
- Virtual Special Issue: Epigenetics 2022.ACS pharmacology & translational science · 2022Article
Corrections and comments
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Authors and funding
13 authors at 5 institutions in 1 country.
Huda ZahidDepartment of Chemistry, University of Minnesota, 207 Pleasant Street SE, Minneapolis, Minnesota 55455, United States.ORCID 0000-0003-1711-7048
Caroline R BuchholzDepartment of Medicinal Chemistry, University of Minnesota, 308 Harvard Street SE, Minneapolis, Minnesota 55455, United States.
Manjulata SinghThe Department of Human and Molecular Genetics, VCU Institute of Molecular Medicine, Massey Cancer Center, Virginia Commonwealth University, Richmond, Virginia 23298, United States.
Michael F CicconeCold Spring Harbor Laboratory, 1 Bungtown Road, Cold Spring Harbor, New York 11724, United States.
Alice ChanDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, 12902 Magnolia Drive, Tampa, Florida 33612, United States.
Stanley NithiananthamDepartment of Chemical Biology & Therapeutics and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Ke ShiDepartment of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, 321 Church Street SE, Minneapolis, Minnesota 55455, United States.ORCID 0000-0003-4175-3714
Hideki AiharaDepartment of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, 321 Church Street SE, Minneapolis, Minnesota 55455, United States.ORCID 0000-0001-7508-6230
Marcus FischerDepartment of Chemical Biology & Therapeutics and Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Ernst SchönbrunnDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, 12902 Magnolia Drive, Tampa, Florida 33612, United States.ORCID 0000-0002-3589-3510
Camila O Dos SantosCold Spring Harbor Laboratory, 1 Bungtown Road, Cold Spring Harbor, New York 11724, United States.
Joseph W LandryThe Department of Human and Molecular Genetics, VCU Institute of Molecular Medicine, Massey Cancer Center, Virginia Commonwealth University, Richmond, Virginia 23298, United States.
William C K PomerantzDepartment of Chemistry, University of Minnesota, 207 Pleasant Street SE, Minneapolis, Minnesota 55455, United States.ORCID 0000-0002-0163-4078
University of Minnesota · USCold Spring Harbor Laboratory · USMoffitt Cancer Center · USSt. Jude Children's Research Hospital · USVirginia Commonwealth University · US
Funding
Single-Cell Biology Shared ResourceP30CA045508 · NCI · COLD SPRING HARBOR LABORATORY · PI David A Tuveson · 1987 to 2026
$118.9MTRANSLATIONAL RESEARCHP30CA076292 · NCI · UNIVERSITY OF SOUTH FLORIDA · PI John L. Cleveland · 1998 to 2026
$93.5MUser Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI STEVEN E EALICK · 2018 to 2026
$34.2MStructural studies of viral replication and invasionR35GM118047 · NIGMS · UNIVERSITY OF MINNESOTA · PI Hideki Aihara · 2016 to 2026
$6.3MTraining the Next Generation of Chemical BiologistsT32GM132029 · NIGMS · UNIVERSITY OF MINNESOTA · PI Erin Elizabeth Carlson, William Charles Krause Pomerantz · 2019 to 2026
$2.7MChemical Probe Development for Epigenetic Complexes Enabled by Protein-Observed 19F NMRR35GM140837 · NIGMS · UNIVERSITY OF MINNESOTA · PI William Charles Krause Pomerantz · 2021 to 2026
$2.5MExploiting Water Network Perturbations in Protein Binding SitesR35GM142772 · NIGMS · ST. JUDE CHILDREN'S RESEARCH HOSPITAL · PI FISCHER, MARCUS · 2021 to 2025
$2.2MProbing the role of epigenomics in Brca1-deficient mammary tumors.R01CA248158 · NCI · COLD SPRING HARBOR LABORATORY · PI DOS SANTOS, CAMILA · 2020 to 2024
$2.2MPixel Array Detector for X-ray CrystallographyS10RR029205 · NCRR · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2010 to 2010
$1.8MDefining the cellular and molecular effects of aging and age of pregnancy on breast tissue homeostasis and cancer initiationR01AG069727 · NIA · COLD SPRING HARBOR LABORATORY · PI DOS SANTOS, CAMILA · 2020 to 2024
$1.8MDefining the Role of BPTF Epigenetic Reader Domains in CancerR01GM121414 · NIGMS · UNIVERSITY OF MINNESOTA · PI POMERANTZ, WILLIAM CHARLES KRAUSE · 2017 to 2020
$1.3MNCI NIH HHS P30 CA045508NCI NIH HHS P30 CA076292NCI NIH HHS R01 CA248158NCRR NIH HHS S10 RR029205NIA NIH HHS R01 AG069727NIGMS NIH HHS P30 GM124165NIGMS NIH HHS R01 GM121414NIGMS NIH HHS R35 GM118047NIGMS NIH HHS R35 GM140837NIGMS NIH HHS R35 GM142772NIGMS NIH HHS T32 GM132029
Abstract
The nucleosome remodeling factor (NURF) alters chromatin accessibility through interactions with its largest subunit,the bromodomain PHD finger transcription factor BPTF. BPTF is overexpressed in several cancers and is an emerging anticancer target. Targeting the BPTF bromodomain presents a potential strategy for its inhibition and the evaluation of its functional significance; however, inhibitor development for BPTF has lagged behind those of other bromodomains. Here we describe the development of pyridazinone-based BPTF inhibitors. The lead compound,
Indexed as
Amino Acid SequenceAnimalsAntigens, NuclearAntineoplastic AgentsBromodomain Containing ProteinsCell Line, TumorDrug DesignMiceMolecular StructureNerve Tissue ProteinsProtein DomainsPyridazinesStructure-Activity RelationshipTranscription FactorsAntigens, NuclearAntineoplastic AgentsBromodomain Containing Proteinsfetal Alzheimer antigenNerve Tissue ProteinsPyridazinesTranscription Factors
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