Therapeutic Targeting of BET Proteins in Sarcoma. [PDF]
Mol Cancer TherAbstract Bromodomain and extraterminal (BET) domain protein family are epigenetic readers that regulate gene transcription, cell-cycle progression, and DNA damage response (DDR), making them attractive therapeutic targets for sarcomas, which are epigenetically dysregulated and genomically unstable.
Riyahi N +8 more
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BET Proteins as Attractive Targets for Cancer Therapeutics. [PDF]
Int J Mol Sci, 2021 Transcriptional dysregulation is a hallmark of cancer and can be an essential driver of cancer initiation and progression. Loss of transcriptional control can cause cancer cells to become dependent on certain regulators of gene expression. Bromodomain and extraterminal domain (BET) proteins are epigenetic readers that regulate the expression of ...
Sarnik J, Popławski T, Tokarz P.
europepmc +4 more sources
The role of BET attenuation in melanoma [PDF]
, 2022 Bromodomain and extra-terminal (BETs) proteins function as epigenetic readers by docking onto acetylated lysine residues (Kac) on histone tails via tandem bromodomains (BRDs), and recruiting protein binding partners via an extra-terminal recruitment ...
Henderson, Elizabeth K
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A Comprehensive Review of BET Protein Biochemistry, Physiology, and Pathological Roles
Frontiers in Pharmacology, 2022 Epigenetic modifications, specifically acetylation of histone plays a decisive role in gene regulation and transcription of normal cellular mechanisms and pathological conditions.
Hafiz Akbar Ali +7 more
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Comparative structure-function analysis of bromodomain and extraterminal motif (BET) proteins in a gene-complementation system [PDF]
Journal of Biological Chemistry, 2020 Joel Mackay +2 more
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Frontiers in Cell and Developmental Biology, 2022 Bromodomain and extra-terminal domain (BET) family proteins play important roles in regulating the expression of multiple proto-oncogenes by recognizing acetylation of histones and non-histone proteins including transcription factors, which subsequently ...
Xiyao Shi +13 more
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Bromodomain protein BRD4 is an epigenetic activator of B7-H6 expression in acute myeloid leukemia
OncoImmunology, 2021 B7-H6, a ligand for the NK activating receptor NKp30, has been identified as a biomarker of poor prognosis in several solid cancers. However, little is known about the role of B7-H6 and the mechanisms that control its expression in acute myeloid leukemia
Aroa Baragaño Raneros +7 more
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BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications
Molecules, 2023 The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes.
Kenneth K. W. To +3 more
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Inhibition of Bromodomain and Extraterminal Domain (BET) Proteins by JQ1 Unravels a Novel Epigenetic Modulation to Control Lipid Homeostasis [PDF]
International Journal of Molecular Sciences, 2020 Giuseppina Caretti +2 more
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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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