ArticleJournal of medicinal chemistry2021
Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy.
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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 12 papers.
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12citing papers in PubMed
2.3field-weighted citation impact, top 11% of its field
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Who cites it
12 citing papers in PubMed, 38 citations in OpenAlex.
- An Integrative Computational Pipeline for CK2 Inhibitor Discovery in Triple-Negative Breast Cancer Using Virtual Screening, Molecular Dynamics, Machine Learning, and Density Functional Theory.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Tandem bromodomains of BRD4 cooperatively read poly-acetylated nucleosomes to enhance chromatin engagement and regulate breast cancer phenotypes.bioRxiv : the preprint server for biology · 2026Article
- Therapeutic Targeting of BET Proteins in Sarcoma.Molecular cancer therapeutics · 2025Review
- Targeting Casein Kinase 2 and Histone Deacetylase with a Dual Inhibitor Effectively Reduces Tumor Growth in a Triple-Negative Breast Cancer Xenograft Model.ACS pharmacology & translational science · 2025Article
- Targeting lysine acetylation readers and writers.Nature reviews. Drug discovery · 2025Review
- Recent Advances in the Discovery of CK2 Inhibitors.ACS omega · 2024Review
- Scoping Pleiotropy of CK2 in Musculoskeletal Disorders for a Novel Targeting Approach.Kinases and phosphatases · 2024Article
- Bromodomain inhibitors and therapeutic applications.Current opinion in chemical biology · 2023Review
- Targeting bromodomain-containing proteins: research advances of drug discovery.Molecular biomedicine · 2023Review
- Pan-cancer molecular subtypes of metastasis reveal distinct and evolving transcriptional programs.Cell reports. Medicine · 2023Article
- CK2 and the Hallmarks of Cancer.Biomedicines · 2022Review
- Preclinical Development of Seriniquinones as Selective Dermcidin Modulators for the Treatment of Melanoma.Marine drugs · 2022Review
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 2 countries.
Jifa ZhangState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Pan TangState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Ling ZouState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Jin ZhangState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Juncheng ChenState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Chengcan YangState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Gu HeState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.ORCID 0000-0002-1536-8882
Bo LiuState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.ORCID 0000-0003-3900-9486
Jie LiuState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Cheng-Ming ChiangSimmons Comprehensive Cancer Center, Department of Pharmacology, and Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.ORCID 0000-0002-4968-3282
Guan WangState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.ORCID 0000-0001-9974-4867
Tinghong YeState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.
Liang OuyangState Key Laboratory of Biotherapy and Cancer Center, Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre, Innovation Center of Nursing Research, Nursing Key Laboratory of Sichuan Province, National Clinical Research Center for Geriatrics, West China Hospital of Sichuan University, Chengdu, 610041 Sichuan, China.ORCID 0000-0001-5537-8834
Sichuan University · CNThe University of Texas Southwestern Medical Center · US
Funding
Opposing Functions of BRD4 Isoforms in Breast CancerR01CA251698 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI CHIANG, CHENG-MING · 2020 to 2024
$2.3MNCI NIH HHS R01 CA251698
Abstract
Bromodomain-containing protein 4 (BRD4) is an attractive epigenetic target in human cancers. Inhibiting the phosphorylation of BRD4 by casein kinase 2 (CK2) is a potential strategy to overcome drug resistance in cancer therapy. The present study describes the synthesis of multiple BRD4-CK2 dual inhibitors based on rational drug design, structure-activity relationship, and
Indexed as
AnimalsAntineoplastic AgentsApoptosisAutophagyBromodomain Containing ProteinsCasein Kinase IICell Cycle ProteinsCell Line, TumorCell ProliferationDrug Screening Assays, AntitumorHumansMiceStructure-Activity RelationshipTranscription FactorsTriple Negative Breast NeoplasmsXenograft Model Antitumor AssaysAntineoplastic AgentsBRD4 protein, humanBromodomain Containing ProteinsCasein Kinase IICell Cycle ProteinsTranscription Factors
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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.