Results 21 to 30 of about 24,956 (275)
BET–HDAC Dual Inhibitors for Combinational Treatment of Breast Cancer and Concurrent Candidiasis
, 2023 Breast cancer is susceptible to Candida infections, and candidiasis has an enhancing effect on the progression and metastasis of tumor. Breast cancer and concurrent candidiasis represent a significant challenge in clinical therapy.
Chunquan Sheng (1364184) +4 more
core +6 more sources
Methylpyrrole inhibitors of BET bromodomains [PDF]
Bioorganic & Medicinal Chemistry Letters, 2017 An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity in a mouse tumor model. Further modifications to the methylpyrrole core provided compounds with improved properties and enhanced ...
Lisa A, Hasvold +27 more
openaire +2 more sources
, 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
Design and characterization of bivalent BET inhibitors [PDF]
Nature Chemical Biology, 2016 Cellular signaling is often propagated by multivalent interactions. Multivalency creates avidity, allowing stable biophysical recognition. Multivalency is an attractive strategy for achieving potent binding to protein targets, as the affinity of bivalent ligands is often greater than the sum of monovalent affinities.
Tanaka, Minoru +8 more
openaire +4 more sources
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
Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies [PDF]
ACS Medicinal Chemistry Letters, 2020 Marcus Frings +2 more
exaly +2 more sources
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
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
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
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