Results 201 to 210 of about 15,581 (231)
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Naphthyridines as Novel BET Family Bromodomain Inhibitors
ChemMedChem, 2013AbstractBromodomains (BRDs) are small protein domains found in a variety of proteins that recognize and bind to acetylated histone tails. This binding affects chromatin structure and facilitates the localisation of transcriptional complexes to specific genes, thereby regulating epigenetically controlled processes including gene transcription and mRNA ...
Olivier, Mirguet +13 more
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BET bromodomain inhibition suppresses adipogenesis in mice
Endocrine, 2019We recently reported that inhibition of BET bromodomain suppresses adipogenesis in vitro. In the present study we aimed to address whether BET bromodomain inhibition can suppress adipogenesis in vivo.Brd4fl/fl mice were crossed with B6.Cg-Tg(Fabp4-cre)1Rev/J mice to generate Brd4fl/+/Fabp4-cre mice.
Qiong Duan +7 more
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Targeting BET bromodomains in hematological malignancies
Hématologie, 2017Les proteines a bromodomaines de la famille BET (pour bromodomain and extra terminal domain) modulent l’expression genique en regulant le controle de l’elongation transcriptionnelle par des elements regulateurs distaux, ou enhancers. Des etudes de criblage fonctionnel et la synthese d’inhibiteurs chimiques ont revele l’importance des proteines BET dans
Justine Penneroux, Raphael Itzykson
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Place your BETs: the therapeutic potential of bromodomains
Trends in Pharmacological Sciences, 2012Therapeutic targeting of the processes that regulate histone modification is a growing area of scientific exploration. Although most interest has concentrated on the various families of enzymes that contribute to these processes, this review focuses on emerging data demonstrating the chemical tractability and therapeutic potential of a hitherto ...
R K, Prinjha, J, Witherington, K, Lee
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Integrative oncology: Addressing the global challenges of cancer prevention and treatment
Ca-A Cancer Journal for Clinicians, 2022Jun J Mao,, Msce +2 more
exaly
DISCOVERING SELECTIVITY IN BET BROMODOMAIN EPIGENETIC REGULATION
The FASEB Journal, 2017Bromodomains are ~110 amino‐acid chromatin interaction modules that bind acetyl‐lysine residues on histones and other nuclear proteins, thereby controlling gene expression through directing assembly of transcriptional complexes on chromatin. The human genome encodes 61 bromodomains distributed among 46 bromodomain‐containing proteins.
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BETting on next-generation bromodomain inhibitors.
American journal of clinical and experimental urologyWithin the last decade, bromodomain and extraterminal (BET) domain inhibitors were introduced as the first in a wave of new agents known as bromodomain inhibitors. These original examples exhibited anti-inflammatory and anticancer properties, and some have progressed to human clinical trials.
Matthew K, Collins +3 more
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BET bromodomains’ functions in bone-related pathologies
2020Throughout life, bones are subjected to the so-called 'bone-remodeling' process, which is a balanced mechanism between the apposition and the resorption of bone. This remodeling process depends on the activities of bone-specialized cells, namely the osteoblasts and the osteoclasts.
Jacques, Camille +7 more
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