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Bromodomain inhibition targeting BPTF in the treatment of melanoma and other solid tumors
Epigenetic mechanisms have been shown to play an important role in the development of cancer. These include the activation of chromatin remodeling...
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The Role of Bromodomain-Containing Proteins in Development and Disease
Purpose of ReviewAn understanding of epigenetic marks on chromatin and their roles in development and disease has been a highlight of the past few...
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A macrophage-cell model of HIV latency reveals the unusual importance of the bromodomain axis
BackgroundAlthough macrophages are now recognized as an essential part of the HIV latent reservoir, whether and how viral latency is established and...
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BET Bromodomain Inhibitors as an Emerging Class of Anticancer Agents
Deregulated gene expression including epigenetic modulation is considered one of the most prominent factors that leads to tumorigenesis, thus...
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Targeting bromodomain-containing proteins: research advances of drug discovery
Bromodomain (BD) is an evolutionarily conserved protein module found in 46 different BD-containing proteins (BCPs). BD acts as a specific reader for...
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The synergistic anticancer effect of the bromodomain inhibitor OTX015 and histone deacetylase 6 inhibitor WT-161 in osteosarcoma
BackgroundOsteosarcoma (OS) is a tumour with a high malignancy level and a poor prognosis. First-line chemotherapy for OS has not been improved for...
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Bromodomain proteins: protectors against endogenous DNA damage and facilitators of genome integrity
Endogenous DNA damage is a major contributor to mutations, which are drivers of cancer development. Bromodomain (BRD) proteins are well-established...
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Distinct modulation of IFNγ-induced transcription by BET bromodomain and catalytic P300/CBP inhibition in breast cancer
BackgroundInterferon gamma (IFNγ) is a pro-inflammatory cytokine that directly activates the JAK/STAT pathway. However, the temporal dynamics of...
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Bromodomain inhibitors a decade later: a promise unfulfilled?
Over the last decade, bromodomain inhibitors have emerged as a promising class of anticancer drugs. However, the clinical progress of these agents...
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Bromodomain inhibitor i-BET858 triggers a unique transcriptional response coupled to enhanced DNA damage, cell cycle arrest and apoptosis in high-grade ovarian carcinoma cells
BackgroundOvarian cancer has a specific unmet clinical need, with a persistently poor 5-year survival rate observed in women with advanced stage...
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Bromodomain-containing protein 4 regulates interleukin-34 expression in mouse ovarian cancer cells
BackgroundInterleukin (IL)-34 acts as an alternative ligand for the colony-stimulating factor-1 receptor and controls the biology of myeloid cells,...
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Inhibition of the bromodomain and extra-terminal family of epigenetic regulators as a promising therapeutic approach for gastric cancer
PurposeEpigenetic dysregulation is a common characteristic of cancers, including gastric cancer (GC), and contributes to cancer development and...
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Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma
BackgroundThe third-generation epithelial growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) have shown significant therapeutic effects on...
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BET bromodomain inhibitors PFI-1 and JQ1 are identified in an epigenetic compound screen to enhance C9ORF72 gene expression and shown to ameliorate C9ORF72-associated pathological and behavioral abnormalities in a C9ALS/FTD model
BackgroundAn intronic GGGGCC (G4C2) hexanucleotide repeat expansion (HRE) in the C9ORF72 gene is the most common cause of amyotrophic lateral...
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Long noncoding RNA HAR1A regulates oral cancer progression through the alpha-kinase 1, bromodomain 7, and myosin IIA axis
AbstractStudies suggested that long noncoding HAR1A RNA may be a tumor suppressor, but its association with oral cancer remains unclear. Here, we...
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A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell lymphoma
BackgroundBromodomain and extra-terminal (BET) proteins are epigenetic readers that can drive carcinogenesis and therapy resistance. RO6870810 is a...
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BRD2 compartmentalizes the accessible genome
Mammalian chromosomes are organized into megabase-sized compartments that are further subdivided into topologically associating domains (TADs). While...
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Dual HDAC–BRD4 inhibitors endowed with antitumor and antihyperalgesic activity
Histone deacetylases (HDAC) are enzymes that regulate the concentration of acetylated histones which, in turns, interact with the bromodomain (BRD)...
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Current and future therapeutic strategies for high-grade gliomas leveraging the interplay between epigenetic regulators and kinase signaling networks
Targeted therapies, including small molecule inhibitors directed against aberrant kinase signaling and chromatin regulators, are emerging treatment...
