BET degrader exhibits lower antiproliferative activity than its inhibitor via EGR1 recruiting septins to promote E2F1-3 transcription in triple-negative breast cancer
Liu N, Wang S, Li M, Zhao N, Wang D, Zhang R, Yu M, Zhao L, Zhang S, Han F, Zhao Y, Liu Q. BET degrader exhibits lower antiproliferative activity than its inhibitor via EGR1 recruiting septins to promote E2F1-3 transcription in triple-negative breast cancer. Pharmacological Research 2024, 208: 107377. PMID: 39209080, DOI: 10.1016/j.phrs.2024.107377.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAntineoplastic AgentsBromodomain Containing ProteinsCell Cycle ProteinsCell Line, TumorCell ProliferationE2F Transcription FactorsE2F1 Transcription FactorE2F3 Transcription FactorEarly Growth Response Protein 1FemaleGene Expression Regulation, NeoplasticHumansMediator Complex Subunit 1MiceMice, NudeTranscription FactorsTranscription, GeneticTriple Negative Breast NeoplasmsConceptsTriple-negative breast cancerBET proteinsRNA polymerase IIBET bromodomainsInhibiting BET proteinsInhibition of cell growthBET degradersBreast cancerPolymerase IIFamily proteinsCell proliferation rate in vitroIncreased Egr1 expressionProliferation rate in vitroBRD4 depletionLysine residuesSeptinE2F1Cell growthRate in vitroExtraterminal domainAntiproliferative activityBET inhibitionProteinEGR1 expressionCell proliferation
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