Results 21 to 30 of about 743,371 (240)
Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy
Signal Transduction and Targeted Therapy, 2023 BET proteins, which influence gene expression and contribute to the development of cancer, are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic anticancer treatment.
Zhi-Qiang Wang +7 more
doaj +1 more source
BET bromodomain inhibitor HMBA synergizes with MEK inhibition in treatment of malignant glioma
Epigenetics, 2021 (1) Background: BET bromodomain proteins regulate transcription by binding acetylated histones and attracting key factors for, e.g., transcriptional elongation.
Elisa Funck-Brentano +3 more
doaj +1 more source
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
doaj +1 more source
Biomolecules, 2020 Currently, proteasome inhibitors bortezomib, carfilzomib, and ixazomib are successfully used in clinics to treat multiple myeloma. However, these agents show limited efficacy against solid tumors. Identification of drugs that can potentiate the action of
Janakiram R. Vangala +2 more
doaj +1 more source
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
doaj +1 more source
Inhibition of BET Family Proteins Suppresses African Swine Fever Virus Infection
Microbiology Spectrum, 2022 African swine fever (ASF), an acute, severe, highly contagious disease caused by African swine fever virus (ASFV) infection in domestic pigs and boars, has a mortality rate of up to 100%.
Yaru Zhao +13 more
doaj +1 more source
Stereoselective synthesis of allele-specific BET inhibitors [PDF]
, 2020 Developing stereoselective synthetic routes that are efficient and cost-effective allows easy access to biologically active molecules. Our previous syntheses of allele-selective bumped inhibitors of the Bromo and Extra-Terminal (BET) domain proteins ...
Testa, Andrea +5 more
core +3 more sources
Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
Nature Communications, 2020 Inhibitors of the BET family proteins are limited by their potency and oral bio-availability. Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous BET inhibitors, and show that it suppresses BRD4 and targets ...
Mingzhu Yin +14 more
doaj +1 more source
, 2022 Bromodomain and extraterminal domain (BET) proteins are important regulators of gene transcription and chromatin remodeling. BET family members BRD4 and BRDT are validated targets for cancer and male contraceptive drug development, respectively.
Narsihmulu Cheryala (13141368) +7 more
core +3 more sources
Stromal fibroblast growth factor 2 reduces the efficacy of bromodomain inhibitors in uveal melanoma
EMBO Molecular Medicine, 2019 Alterations in transcriptional programs promote tumor development and progression and are targetable by bromodomain and extraterminal (BET) protein inhibitors.
Vivian Chua +12 more
doaj +1 more source