Roles of Bromodomain Extra Terminal Proteins in Metabolic Signaling and Diseases
Pharmaceuticals, 2022 BET proteins, which recognize and bind to acetylated histones, play a key role in transcriptional regulation. The development of chemical BET inhibitors in 2010 greatly facilitated the study of these proteins.
Dayu Wu, Qiong Duan
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Roles of reconstituted high-density lipoprotein nanoparticles in cardiovascular disease: A new paradigm for drug discovery [PDF]
, 2020 Epidemiological results revealed that there is an inverse correlation between high-density lipoprotein (HDL) cholesterol levels and risks of atherosclerotic cardiovascular disease (ASCVD).
Huang, Hui +3 more
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Targeting MYCN-Driven Transcription By BET-Bromodomain Inhibition [PDF]
Clinical Cancer Research, 2016 Abstract Purpose: Targeting BET proteins was previously shown to have specific antitumoral efficacy against MYCN-amplified neuroblastoma. We here assess the therapeutic efficacy of the BET inhibitor, OTX015, in preclinical neuroblastoma models and extend the knowledge on the role of BRD4 in MYCN-driven neuroblastoma.
Henssen, Anton +22 more
openaire +3 more sources
TRPM3-Induced Gene Transcription Is under Epigenetic Control
Pharmaceuticals, 2022 Transient receptor potential M3 (TRPM3) cation channels regulate numerous biological functions, including gene transcription. Stimulation of TRPM3 channels with pregnenolone sulfate activates stimulus-responsive transcription factors, which bind to short
Gerald Thiel, Oliver G. Rössler
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Clinical progress and pharmacology of small molecule bromodomain inhibitors [PDF]
, 2016 Bromodomains have emerged as an exciting target class for drug discovery over the past decade. Research has primarily focused on the bromodomain and extra terminal (BET) family of bromodomains, which has led to the development of multiple small molecule ...
Humphreys, Philip G +3 more
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A Novel t(8;14)(q24;q11) Rearranged Human Cell Line as a Model for Mechanistic and Drug Discovery Studies of NOTCH1-Independent Human T-Cell Leukemia [PDF]
, 2018 MYC-translocated T-lineage acute lymphoblastic leukemia (T-ALL) is a rare subgroup of T-ALL associated with CDKN2A/B deletions, PTEN inactivation, and absence of NOTCH1 or FBXW7 mutations.
Amadori, Alberto +12 more
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Data in Brief, 2016 Apabetalone (RVX-208) inhibits the interaction between epigenetic regulators known as bromodomain and extraterminal (BET) proteins and acetyl-lysine marks on histone tails. Data presented here supports the manuscript published in Atherosclerosis “RVX-208,
Sylwia Wasiak +12 more
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Application of Small Epigenetic Modulators in Pediatric Medulloblastoma [PDF]
, 2018 Medulloblastoma is one of the most frequent among pediatric brain tumors, and it has been classified in various subgroups. Some of them already benefit from quite good therapeutic options, whereas others urgently need novel therapeutic approaches ...
Annalisa Romanelli +8 more
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Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition [PDF]
, 2018 Allele-specific chemical genetics enables selective inhibition within families of highly-conserved proteins. The four BET (bromodomain & extra-terminal domain) proteins – BRD2, BRD3, BRD4 and BRDT bind acetylated chromatin via their bromodomains and ...
Albrecht +59 more
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Cell Reports, 2013 A hallmark of retroviral replication is integration of the viral genome into host cell DNA. This characteristic makes retrovirus-based vectors attractive delivery vehicles for gene therapy.
Jan De Rijck +11 more
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