[HTML][HTML] Targeting multiple signaling pathways: the new approach to acute myeloid leukemia therapy

JL Carter, K Hege, J Yang, HA Kalpage, Y Su… - Signal transduction and …, 2020 - nature.com
Acute myeloid leukemia (AML) is the most common form of acute leukemia in adults and the
second most common form of acute leukemia in children. Despite this, very little …

[HTML][HTML] Protein acylation: mechanisms, biological functions and therapeutic targets

S Shang, J Liu, F Hua - Signal Transduction and Targeted Therapy, 2022 - nature.com
Metabolic reprogramming is involved in the pathogenesis of not only cancers but also
neurodegenerative diseases, cardiovascular diseases, and infectious diseases. With the …

BET bromodomain inhibitors

MP Schwalm, S Knapp - Current opinion in chemical biology, 2022 - Elsevier
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain
proteins that have emerged as principal regulators of linage specific gene transcription. The …

TP63, SOX2, and KLF5 establish a core regulatory circuitry that controls epigenetic and transcription patterns in esophageal squamous cell carcinoma cell lines

YY Jiang, Y Jiang, CQ Li, Y Zhang, P Dakle, H Kaur… - Gastroenterology, 2020 - Elsevier
Background & Aims We investigated the transcriptome of esophageal squamous cell
carcinoma (ESCC) cells, activity of gene regulatory (enhancer and promoter regions), and …

[HTML][HTML] Stromal induction of BRD4 phosphorylation results in chromatin remodeling and BET inhibitor resistance in colorectal cancer

W Wang, YA Tang, Q Xiao, WC Lee, B Cheng… - Nature …, 2021 - nature.com
BRD4, a Bromodomain and Extraterminal (BET) protein family member, is a promising anti-
cancer drug target. However, resistance to BET inhibitors targeting BRD4 is common in solid …

Targeting Brd4 for cancer therapy: inhibitors and degraders

Y Duan, Y Guan, W Qin, X Zhai, B Yu, H Liu - Medchemcomm, 2018 - pubs.rsc.org
Bromodomain-containing protein 4 (Brd4) plays an important role in mediating the
expression of genes involved in cancers and non-cancer diseases such as inflammatory …

Multi-omics reveals clinically relevant proliferative drive associated with mTOR-MYC-OXPHOS activity in chronic lymphocytic leukemia

J Lu, E Cannizzaro, F Meier-Abt, S Scheinost… - Nature cancer, 2021 - nature.com
Chronic lymphocytic leukemia (CLL) has a complex pattern of driver mutations and much of
its clinical diversity remains unexplained. We devised a method for simultaneous subgroup …

Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744) …

GS Sheppard, L Wang, SD Fidanze… - Journal of Medicinal …, 2020 - ACS Publications
The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains
two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under …

[HTML][HTML] Enhancer architecture and essential core regulatory circuitry of chronic lymphocytic leukemia

CJ Ott, AJ Federation, LS Schwartz, S Kasar… - Cancer cell, 2018 - cell.com
Enhancer profiling is a powerful approach for discovering cis-regulatory elements that define
the core transcriptional regulatory circuits of normal and malignant cells. Gene control …

BET proteins: Biological functions and therapeutic interventions

J Guo, Q Zheng, Y Peng - Pharmacology & Therapeutics, 2023 - Elsevier
Bromodomain and extra-terminal (BET) family member proteins (BRD2, BRD3, BRD4 and
BRDT) play a pivotal role in interpreting the epigenetic information of histone Kac …