ArticleCancer medicine2019
BET inhibitor JQ1 suppresses cell proliferation via inducing autophagy and activating LKB1/AMPK in bladder cancer cells.
Article in Cancer medicine, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 48 citations in OpenAlex.
- Targeting pre-existing club-like cells in prostate cancer potentiates androgen deprivation therapy.EMBO molecular medicine · 2026Article
- An overview of autophagy inhibition as a potential clinical strategy in cancer therapy.Molecular pharmacology · 2025Review
- ZC3H13 promotes autophagy in bladder cancer through m6A methylation modification of PJA2 and ubiquitination of KSR1.Human cell · 2024Article
- Honokiol relieves hippocampal neuronal damage in Alzheimer's disease by activating the SIRT3-mediated mitochondrial autophagy.CNS neuroscience & therapeutics · 2024Article
- JQ1 attenuates contrast-induced acute kidney injury through the upregulation of autophagy and inhibition of inflammation.International urology and nephrology · 2024Article
- Critical roles of lncRNA-mediated autophagy in urologic malignancies.Frontiers in pharmacology · 2024Review
- A new vulnerability to BET inhibition due to enhanced autophagy in BRCA2 deficient pancreatic cancer.Cell death & disease · 2023Article
- Cytoprotective, Cytotoxic and Cytostatic Roles of Autophagy in Response to BET Inhibitors.International journal of molecular sciences · 2023Review
- Bromodomain and Extraterminal Domain (BET) Protein Inhibition Hinders Glioblastoma Progression by Inducing Autophagy-Dependent Differentiation.International journal of molecular sciences · 2023Article
- Review
- FLI1 and FRA1 transcription factors drive the transcriptional regulatory networks characterizing muscle invasive bladder cancer.Communications biology · 2023Article
- Non-apoptotic cell death-based cancer therapy: Molecular mechanism, pharmacological modulators, and nanomedicine.Acta pharmaceutica Sinica. B · 2022Review
- BET protein inhibition in macrophages enhances dorsal root ganglion neurite outgrowth in female mice.Journal of neuroscience research · 2022Article
- Autophagy regulation by RNA alternative splicing and implications in human diseases.Nature communications · 2022Review
- Autophagy-related signaling pathways are involved in cancer (Review).Experimental and therapeutic medicine · 2021Review
- Epigenetic regulation of autophagy: A key modification in cancer cells and cancer stem cells.World journal of stem cells · 2021Review
- Epigenomic and Metabolomic Integration Reveals Dynamic Metabolic Regulation in Bladder Cancer.Cancers · 2021Review
- Contrast effects of autophagy in the treatment of bladder cancer.Experimental biology and medicine (Maywood, N.J.) · 2021Review
- Crucial Roles of microRNA-Mediated Autophagy in Urologic Malignancies.International journal of biological sciences · 2021Review
- Advances in the pathogenesis and treatment of nut carcinoma: a narrative review.Translational cancer research · 2020Review
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimJQ1, a BET bromodomain inhibitor, is a promising therapeutic approach for bladder cancer (BC). Our study aimed to determine whether autophagy is induced by JQ1 and its potential role toward proliferation in BC.
methodsCell proliferation was determined by methylthiazolyldiphenyl-tetrazolium bromide (MTT) assay, cell counting assay, and colony formation assay. Autophagosomes and autolysosomes were observed by transmission electron microscopy and mRFP-EGFP-LC3 fluorescence assay. 3-MA, BAFA1, NH
resultsWe found that BC cell proliferation was suppressed by JQ1; moreover, JQ1 induced the accumulation of autophagosomes and autolysosomes, and autophagy flux, and the growth suppression capacity of JQ1 was attenuated by autophagy inhibitors. Furthermore, we found that JQ1 induced the phosphorylation of AMPKα, and AMPKα knockdown attenuated autophagy induction and anti-proliferation effect induced by JQ1 in BC cells, indicating that autophagy induced by JQ1 is dependent on AMPKα. Through endogenous immunoprecipitation analysis, we found that JQ1 dramatically increased the interaction between LKB1 and AMPKα, which may lead to more AMPK activation. Proliferation inhibition, autophagy induction, and LKB1/AMPK activation capacities of JQ1 were further confirmed in vivo.
conclusionsTaken together, our results demonstrate that autophagy is induced by JQ1 through activation of LKB1/AMPK pathway, and the autophagy induced by JQ1 positively contributes to the inhibition of BC cell proliferation. These findings provide a novel point of view to understand the mechanism of how targeting BET bromodomain suppress cancer cell growth and suggest that targeting BET bromodomain might be a potential approach to treat BC in the future.
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