Small-Molecule Dual PLK1 and BRD4 Inhibitors are Active Against Preclinical Models of Pediatric Solid Tumors
Timme N, Han Y, Liu S, Yosief H, GarcÃa 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 regulatorSynergistic activity of BET inhibitor MK-8628 and PLK inhibitor Volasertib in preclinical models of medulloblastoma
Han Y, Lindner S, Bei Y, Garcia H, Timme N, Althoff K, Odersky A, Schramm A, Lissat A, Künkele A, Deubzer H, Eggert A, Schulte J, Henssen A. Synergistic activity of BET inhibitor MK-8628 and PLK inhibitor Volasertib in preclinical models of medulloblastoma. Cancer Letters 2019, 445: 24-33. PMID: 30611741, DOI: 10.1016/j.canlet.2018.12.012.Peer-Reviewed Original ResearchConceptsModel of medulloblastomaMYC-amplified medulloblastomaMK-8628Preclinical models of medulloblastomaAnti-tumor effectsPreclinical modelsTherapeutic efficacyCentral nervous system tumorsAggressive clinical courseHigh-risk medulloblastomaTherapy-related morbidityCurrent treatment regimensNervous system tumorsTargeted treatment approachesBET protein BRD4MYC protein stabilityIn vivo modelsMYC amplificationMedulloblastoma modelApoptotic cell deathCell cycle arrestClinical courseTreatment regimensSystem tumorsTarget of Plk1
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