Bromodomain biology and drug discovery
N Zaware, MM Zhou - Nature structural & molecular biology, 2019 - nature.com
The bromodomain (BrD) is a conserved structural module found in chromatin-and
transcription-associated proteins that acts as the primary reader for acetylated lysine …
transcription-associated proteins that acts as the primary reader for acetylated lysine …
Bromodomain and extra-terminal motif inhibitors: a review of preclinical and clinical advances in cancer therapy
A Alqahtani, K Choucair, M Ashraf… - Future science …, 2019 - Taylor & Francis
Histone lysine acetylation is critical in regulating transcription. Dysregulation of this process
results in aberrant gene expression in various diseases, including cancer. The …
results in aberrant gene expression in various diseases, including cancer. The …
[HTML][HTML] A chemical toolbox for the study of bromodomains and epigenetic signaling
Bromodomains (BRDs) are conserved protein interaction modules which recognize (read)
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …
Molecules targeting the androgen receptor (AR) signaling axis beyond the AR‐Ligand binding domain
NGRD Elshan, MB Rettig… - Medicinal research reviews, 2019 - Wiley Online Library
Prostate cancer (PCa) is the second most common cause of cancer‐related mortality in men
in the United States. The androgen receptor (AR) and the physiological pathways it …
in the United States. The androgen receptor (AR) and the physiological pathways it …
[HTML][HTML] Pharmacological targeting of BET bromodomain proteins in acute myeloid leukemia and malignant lymphomas: from molecular characterization to clinical …
D Reyes-Garau, ML Ribeiro, G Roué - Cancers, 2019 - mdpi.com
Alterations in protein-protein and DNA-protein interactions and abnormal chromatin
remodeling are a major cause of uncontrolled gene transcription and constitutive activation …
remodeling are a major cause of uncontrolled gene transcription and constitutive activation …
[HTML][HTML] The repositioning of epigenetic probes/inhibitors identifies new anti-schistosomal lead compounds and chemotherapeutic targets
KCL Whatley, G Padalino, H Whiteland… - PLoS Neglected …, 2019 - journals.plos.org
Background Praziquantel represents the frontline chemotherapy used to treat
schistosomiasis, a neglected tropical disease (NTD) caused by infection with macro …
schistosomiasis, a neglected tropical disease (NTD) caused by infection with macro …
Chemical proteomic profiling of bromodomains enables the wide-spectrum evaluation of bromodomain inhibitors in living cells
X Li, Y Wu, G Tian, Y Jiang, Z Liu, X Meng… - Journal of the …, 2019 - ACS Publications
Bromodomains, epigenetic “readers” of lysine acetylation marks, exist in different nuclear
proteins with diverse biological functions in chromatin biology. Malfunctions of …
proteins with diverse biological functions in chromatin biology. Malfunctions of …
Discovery of selective inhibitors for cyclic AMP response element-binding protein: A combined ligand and structure-based resources pipeline
I Muneer, MT ul Qamar, K Tusleem, SA Rauf… - Anti-Cancer …, 2019 - journals.lww.com
Bromodomains are epigenetic readers of acetyl-lysine involved in chromatin remodeling
and transcriptional regulations. Over the past few years, extensive research has been …
and transcriptional regulations. Over the past few years, extensive research has been …
Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation
M Schiedel, M Moroglu, DMH Ascough… - Angewandte Chemie …, 2019 - Wiley Online Library
Epigenetics is currently the focus of intense research interest across a broad range of
disciplines due to its importance in a multitude of biological processes and disease states …
disciplines due to its importance in a multitude of biological processes and disease states …
The bromodomain protein BRD4 positively regulates necroptosis via modulating MLKL expression
Y Xiong, L Li, L Zhang, Y Cui, C Wu, H Li… - Cell Death & …, 2019 - nature.com
Necroptosis is a programmed form of necrotic cell death, which is tightly regulated by the
necroptotic signaling pathway containing receptor-interacting protein (RIP) 1, RIP3, and …
necroptotic signaling pathway containing receptor-interacting protein (RIP) 1, RIP3, and …