2022
BRD4 inhibitor suppresses melanoma metastasis via the SPINK6/EGFR-EphA2 pathway
Hu R, Li Y, Guo Y, Li X, Du S, Liao M, Hou H, Sun H, Zhao S, Su J, Chen X, Yin M. BRD4 inhibitor suppresses melanoma metastasis via the SPINK6/EGFR-EphA2 pathway. Pharmacological Research 2022, 187: 106609. PMID: 36516883, DOI: 10.1016/j.phrs.2022.106609.Peer-Reviewed Original Research
2020
Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
Yin M, Guo Y, Hu R, Cai WL, Li Y, Pei S, Sun H, Peng C, Li J, Ye R, Yang Q, Wang N, Tao Y, Chen X, Yan Q. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nature Communications 2020, 11: 1833. PMID: 32286255, PMCID: PMC7156724, DOI: 10.1038/s41467-020-15290-0.Peer-Reviewed Original ResearchMeSH KeywordsAdministration, OralAnimalsCell CommunicationCell Cycle ProteinsCell Line, TumorCell ProliferationDisease Models, AnimalDown-RegulationDrug DesignFemaleHumansHypoxia-Inducible Factor 1, alpha SubunitMacrophage Colony-Stimulating FactorMacrophagesMice, Inbred BALB CMice, NudeNeoplasmsPhosphorylationProto-Oncogene Proteins c-mycReceptors, Granulocyte-Macrophage Colony-Stimulating FactorSignal TransductionTranscription FactorsTreatment OutcomeConceptsTumor growthMajor clinical stagesBET inhibitorsProliferation of tumorsExtraterminal domain (BET) family proteinsTumor cell proliferationClinical stageTumor shrinkageSyngeneic modelPotent BRD4 inhibitorsSmall molecule inhibitorsSolid tumorsBRD4 inhibitionTumor cellsOral bioavailabilityCancer treatmentCell proliferationBRD4 inhibitorsMolecule inhibitorsMultiple mechanismsC-MycTumorsInhibitors
2019
Small-Molecule Dual PLK1 and BRD4 Inhibitors are Active Against Preclinical Models of Pediatric Solid Tumors
Timme N, Han Y, Liu S, Yosief H, García H, Bei Y, Klironomos F, MacArthur I, Szymansky A, von Stebut J, Bardinet V, Dohna C, Künkele A, Rolff J, Hundsdörfer P, Lissat A, Seifert G, Eggert A, Schulte J, Zhang W, Henssen A. Small-Molecule Dual PLK1 and BRD4 Inhibitors are Active Against Preclinical Models of Pediatric Solid Tumors. Translational Oncology 2019, 13: 221-232. PMID: 31869746, PMCID: PMC6931204, DOI: 10.1016/j.tranon.2019.09.013.Peer-Reviewed Original ResearchPediatric tumor cell linesTumor cell linesTreatment of patient-derived xenograftsClinical response to therapySignificant tumor regressionPediatric solid tumorsResponse to therapyPatient-derived xenograftsPediatric cancer modelsTumor-specific activationCell linesRhabdomyosarcoma tumor cellsTumor regressionPreclinical modelsSolid tumorsAntitumor effectCancer modelsTumor cellsConcurrent inhibitionAntitumor activityInduce apoptosisSimultaneous inhibitionMolecular targetsBRD4 inhibitorsCentral regulator
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