BET‐ting on Nrf2: How Nrf2 Signaling can Influence the Therapeutic Activities of BET Protein Inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "BioEssays"
DOI: 10.1002/bies.201800007
Abstract: BET proteins such as Brd3 and Brd4 are chromatin‐associated factors, which control gene expression programs that promote inflammation and cancer. The Nrf2 transcription factor is a master regulator of genes that protect the organism against… read more here.
Keywords: nrf2 bet; bet proteins; ting nrf2; bet ting ... See more keywords
Selective inhibitors of bromodomain BD1 and BD2 of BET proteins modulate radiation‐induced profibrotic fibroblast responses
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Cancer"
DOI: 10.1002/ijc.33989
Abstract: Radiotherapy can induce various adverse effects including fibrosis in cancer patients. Radiation‐induced aberrant expression of profibrotic genes has been associated with dysregulated epigenetic mechanisms. Pan‐BET (bromodomain and extraterminal domain) inhibitors, such as JQ1 and I‐BET151,… read more here.
Keywords: bet proteins; bd2; ibet bd2; radiation induced ... See more keywords
Emerging roles of and therapeutic strategies targeting BRD4 in cancer.
Sign Up to like & getrecommendations! Published in 2019 at "Cellular immunology"
DOI: 10.1016/j.cellimm.2019.02.001
Abstract: The Bromodomain and Extra-terminal (BET) family of proteins were first recognized as important epigenetic regulators in inflammatory processes; however, there is increasing evidence to support the notion that BET proteins also play a critical role… read more here.
Keywords: bet proteins; emerging roles; strategies targeting; therapeutic strategies ... See more keywords
BET protein inhibition promotes non-myeloid cell mediated neuroprotection after rodent spinal cord contusion
Sign Up to like & getrecommendations! Published in 2022 at "Experimental Neurology"
DOI: 10.1016/j.expneurol.2022.114035
Abstract: Spinal cord injuries (SCI) often lead to multiple neurological deficits as a result from the initial trauma and also the secondary damage that follows. Despite abundant preclinical data proposing anti-inflammatory therapies to minimize secondary injury… read more here.
Keywords: bet; inhibition; bet protein; bet proteins ... See more keywords
BET proteins inhibitor JQ-1 impaired the extinction of remote auditory fear memory: An effect mediated by insulin like growth factor 2
Sign Up to like & getrecommendations! Published in 2020 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2020.108255
Abstract: Fear extinction is an important preclinical model for behavior therapy in human anxiety disorders, such as post-traumatic stress disorder (PTSD). Histone acetylation is involved in the extinction of fear memory. As the "readers" of histone… read more here.
Keywords: extinction remote; bet proteins; extinction; auditory fear ... See more keywords
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01835
Abstract: Blocking the interactions between bromodomain and extraterminal (BET) proteins and acetylated lysines of histones by small molecules has important implications for the treatment of cancers and other diseases. Many pan-BET inhibitors have shown satisfactory results… read more here.
Keywords: bet; development; selective inhibitors; bromodomain ... See more keywords
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.6b01816
Abstract: The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are considered to… read more here.
Keywords: extra terminal; bet proteins; small molecule; bet ... See more keywords
BET inhibitors: a novel epigenetic approach
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DOI: 10.1093/annonc/mdx157
Abstract: Epigenetics has been defined as 'the structural adaptation of chromosomal regions so as to register, signal or perpetuate altered activity states.' Currently, several classes of anticancer drugs function at the epigenetic level, including inhibitors of… read more here.
Keywords: bet proteins; inhibitors novel; approach; epigenetic approach ... See more keywords
BET Proteins: An Approach to Future Therapies in Transplantation
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DOI: 10.1111/ajt.14221
Abstract: In order to develop new efficient therapies for organ transplantation, it is essential to acquire a comprehensive knowledge of the molecular mechanisms and processes, such as immune activation, chronic inflammation, and fibrosis, which lead to… read more here.
Keywords: bet proteins; therapies transplantation; transplantation bet; proteins approach ... See more keywords
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
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DOI: 10.1126/science.aaz8455
Abstract: Bromodomain inhibitors revisited Bromodomain and extraterminal domain (BET) proteins contribute to the pathogenesis of cancer and immune diseases through their effects on transcriptional regulation. BET proteins contain two nearly identical bromodomains, BD1 and BD2, structural… read more here.
Keywords: bd1 bd2; bet; cancer; bet proteins ... See more keywords
BET Proteins Exhibit Transcriptional and Functional Opposition in the Epithelial-to-Mesenchymal Transition
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DOI: 10.1158/1541-7786.mcr-17-0568
Abstract: Transcriptional programs in embryogenesis and cancer, such as the epithelial-to-mesenchymal transition (EMT), ensure cellular plasticity, an essential feature of carcinoma progression. As effectors of signal transduction, the bromodomain and extraterminal (BET) proteins are well suited… read more here.
Keywords: mesenchymal transition; bet proteins; bet; epithelial mesenchymal ... See more keywords