Results 51 to 60 of about 104,722 (190)
Neoplasia: An International Journal for Oncology Research, 2022 BH3 mimetics are promising novel anticancer therapeutics. By selectively inhibiting BCL-2, BCL-xL, or MCL-1 (i.e. ABT-199, A-1331852, S63845) they shift the balance of pro- and anti-apoptotic proteins in favor of apoptosis.
Ufuk Erdogdu +7 more
doaj +1 more source
BRD4-BRD2 isoform switching coordinates pluripotent exit and Smad2-dependent lineage specification [PDF]
, 2017 Pluripotent Stem Cells (PSCs) hold great clinical potential, as they possess the capacity to differentiate into fully specialised tissues such as pancreas, liver, neurons and cardiac muscle.
Ciulli, Alessio +8 more
core +3 more sources
BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms [PDF]
Leukemia, 2013 Small molecule inhibition of the BET family of proteins, which bind acetylated lysines within histones, has been shown to have a marked therapeutic benefit in pre-clinical models of mixed lineage leukemia (MLL) fusion protein-driven leukemias. Here, we report that I-BET151, a highly specific BET family bromodomain inhibitor, leads to growth inhibition ...
B S Wyspiańska +16 more
openaire +4 more sources
Epigenetics & Chromatin, 2019 Background Deregulated transcription is a major driver of diseases such as cancer. Bromodomain and extra-terminal (BET) proteins (BRD2, BRD3, BRD4 and BRDT) are chromatin readers essential for maintaining proper gene transcription by specifically binding
P. Khoueiry +11 more
doaj +1 more source
Transcriptional repressor ZEB2 promotes terminal differentiation of CD8⁺ effector and memory T cell populations during infection [PDF]
, 2015 ZEB2 is a multi-zinc-finger transcription factor known to play a significant role in early neurogenesis and in epithelial-mesenchymal transition-dependent tumor metastasis.
Agata Stryjewska +72 more
core +3 more sources
Structure of the Brd4 ET domain bound to a C-terminal motif from γ-retroviral integrases reveals a conserved mechanism of interaction [PDF]
, 2016 The bromodomain and extraterminal domain (BET) protein family are promising therapeutic targets for a range of diseases linked to transcriptional activation, cancer, viral latency, and viral integration.
Crowe, Brandon L. +5 more
core +2 more sources
Selective Inhibition of BET Protein Domains Has Functional Relevance [PDF]
Cancer Discovery, 2020 Abstract Inhibition of BET protein bromodomains BD1 and BD2 produces unique phenotypes in disease models.
openaire +2 more sources
EWS/ETS-Driven Ewing Sarcoma Requires BET Bromodomain Proteins [PDF]
Cancer Research, 2018 Abstract The EWS/ETS fusion transcription factors drive Ewing sarcoma (EWS) by orchestrating an oncogenic transcription program. Therapeutic targeting of EWS/ETS has been unsuccessful; however, identifying mediators of the EWS/ETS function could offer new therapeutic options.
Paradesi Naidu, Gollavilli +12 more
openaire +2 more sources
Exploration of Targeted Anti-tumor Therapy, 2021 Aim: Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that play a fundamental role in transcription regulation. Preclinical and early clinical evidence sustain BET targeting as an anti-cancer approach.
Chiara Tarantelli +14 more
doaj +1 more source
Cancer Differentiating Agent Hexamethylene Bisacetamide Inhibits BET Bromodomain Proteins [PDF]
Cancer Research, 2016 Abstract Agents that trigger cell differentiation are highly efficacious in treating certain cancers, but such approaches are not generally effective in most malignancies. Compounds such as DMSO and hexamethylene bisacetamide (HMBA) have been used to induce differentiation in experimental systems, but their mechanisms of action and ...
Lisa M, Nilsson +8 more
openaire +2 more sources