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BRD4 inhibitor GNE987 exerts anti-cancer effects in Neuroblastoma (ChIP-Seq)

ABSTRACT: BRD4 inhibitor GNE987 exerts anti-cancer effects in Neuroblastoma (ChIP-Seq)

PROVIDER: PRJNA800647 | ENA |

REPOSITORIES: ENA

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			Action	DRS
	SRR17760985.fastq.gz	Fastqsanger.gz
	SRR17760986.fastq.gz	Fastqsanger.gz

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BRD4 inhibitor GNE987 exerts anti-cancer effects in Neuroblastoma

Project description:Neuroblastoma (NB) is the most common extracranial solid tumor of childhood, which is derived from primordial neural crest cells. GNE987 is a newly developed von Hippel-Lindau tumor suppressor (VHL)-based pan-BET-targeting PROTAC, which can bind to the target proteins (BET proteins, including BRD2, BRD3, and BRD4) and recruit them to the ubiquitin/ proteasome system for selective degradation. However, the function of GNE987 has not been assessed in NB models so far. In the present study, RNA-seq analysis was performed to explore the effect of GNE987 on NB cells.

2022-03-23 | GSE190002 | GEO

BRD4 inhibitor GNE987 exerts anti-cancer effects in Neuroblastoma

Project description:BRD4 inhibitor GNE987 exerts anti-cancer effects in Neuroblastoma

| PRJNA785569 | ENA

BRD4 inhibitor GNE987 exerts anti-cancer effects in Neuroblastoma (ChIP-Seq)

Project description:Neuroblastoma (NB) is the most common extracranial solid tumor of childhood, which is derived from primordial neural crest cells. GNE987 is a newly developed von Hippel-Lindau tumor suppressor (VHL)-based pan-BET-targeting PROTAC, which can bind to the target proteins (BET proteins, including BRD2, BRD3, and BRD4) and recruit them to the ubiquitin/ proteasome system for selective degradation. However, the function of GNE987 has not been assessed in NB models so far. In the present study, ChIP-Seq analysis was performed to explore the effect of GNE987 on NB cells.

2022-03-23 | GSE194430 | GEO

BRD4 inhibitor GNE987 exerts anti-cancer effects in Osteosarcoma

Project description:GNE987 is a newly developed von Hippel-Lindau tumor suppressor (VHL)-based pan-BET-targeting PROTAC, which can bind to the target proteins (BET proteins, including BRD2, BRD3, and BRD4) and recruit them to the ubiquitin/proteasome system for selective degradation. In the our study, ChIP-Seq analysis was performed to explore the effect of GNE987 on osteosarcoma cells.

2024-08-08 | GSE243673 | GEO

BRD4 inhibitor GNE987 exerts anti-cancer effects in Osteosarcoma

Project description:BRD4 inhibitor GNE987 exerts anti-cancer effects in Osteosarcoma

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BRD4 inhibitor MZ1 exerts anti-cancer effects in Neuroblastoma

Project description:BRD4 inhibitor MZ1 exerts anti-cancer effects in Neuroblastoma

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BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting C-Myc and S100A16 in Glioblastoma [ChIP-seq]

Project description:Glioblastoma (GBM) in children is a relatively more common primary central nervous system tumor with a high degree of malignancy, high mortality, and complex surgical complete resection.. GNE987 is a newly developed von Hippel-Lindau tumor suppressor (VHL)-based pan-BET-targeting PROTAC, which can bind to the target proteins (BET proteins, including BRD2, BRD3, and BRD4) and recruit them to the ubiquitin/ proteasome system for degradation. However, the function of GNE987 has not been assessed in GBM cells so far. In the present study, ChIP-Seq analysis was performed to explore the effect of GNE987 on GBM cells.

2022-11-09 | GSE202484 | GEO

BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting C-Myc and S100A16 in Glioblastoma

Project description:To investigate the function of GNE987 in the regulation of gene expression, we treated U87 cells with control (DMSO) or GNE987, respectively. We then performed gene expression profiling analysis using data obtained from RNA-seq of control and GNE987 treatment.

2022-11-09 | GSE202362 | GEO

BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting super-enhancers in neuroblastoma.

Project description:BackgroundNeuroblastoma (NB) is a common extracranial malignancy with high mortality in children. Recently, super-enhancers (SEs) have been reported to play a critical role in the tumorigenesis and development of NB via regulating a wide range of oncogenes Thus, the synthesis and identification of chemical inhibitors specifically targeting SEs are of great urgency for the clinical therapy of NB. This study aimed to characterize the activity of the SEs inhibitor GNE987, which targets BRD4, in NB.ResultsIn this study, we found that nanomolar concentrations of GNE987 markedly diminished NB cell proliferation and survival via degrading BRD4. Meanwhile, GNE987 significantly induced NB cell apoptosis and cell cycle arrest. Consistent with in vitro results, GNE987 administration (0.25 mg/kg) markedly decreased the tumor size in the xenograft model, with less toxicity, and induced similar BRD4 protein degradation to that observed in vitro. Mechanically, GNE987 led to significant downregulation of hallmark genes associated with MYC and the global disruption of the SEs landscape in NB cells. Moreover, a novel candidate oncogenic transcript, FAM163A, was identified through analysis of the RNA-seq and ChIP-seq data. FAM163A is abnormally transcribed by SEs, playing an important role in NB occurrence and development.ConclusionGNE987 destroyed the abnormal transcriptional regulation of oncogenes in NB by downregulating BRD4, which could be a potential therapeutic candidate for NB.

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BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting C-Myc and S100A16 in Glioblastoma

Project description:BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting C-Myc and S100A16 in Glioblastoma

| PRJNA835712 | ENA