Targeting bromodomains: epigenetic readers of lysine acetylation
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …
Protein lysine acetylation by p300/CBP
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …
[HTML][HTML] BET inhibitors: a novel epigenetic approach
Epigenetics has been defined as 'the structural adaptation of chromosomal regions so as to
register, signal or perpetuate altered activity states.'Currently, several classes of anticancer …
register, signal or perpetuate altered activity states.'Currently, several classes of anticancer …
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 …
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
S Picaud, C Wells, I Felletar… - Proceedings of the …, 2013 - National Acad Sciences
Bromodomains have emerged as attractive candidates for the development of inhibitors
targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently …
targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently …
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 …
Chromatin proteins and modifications as drug targets
K Helin, D Dhanak - Nature, 2013 - nature.com
A plethora of groundbreaking studies have demonstrated the importance of chromatin-
associated proteins and post-translational modifications of histones, proteins and DNA (so …
associated proteins and post-translational modifications of histones, proteins and DNA (so …
Bromodomain inhibitors and cancer therapy: From structures to applications
M Pérez-Salvia, M Esteller - Epigenetics, 2017 - Taylor & Francis
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes
that are “writers,”“erasers,” or “readers” of histone modification marks are common …
that are “writers,”“erasers,” or “readers” of histone modification marks are common …
BET bromodomains mediate transcriptional pause release in heart failure
Heart failure (HF) is driven by the interplay between regulatory transcription factors and
dynamic alterations in chromatin structure. Pathologic gene transactivation in HF is …
dynamic alterations in chromatin structure. Pathologic gene transactivation in HF is …
Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
Small molecule inhibitor of the bromodomain and extraterminal domain (BET) family
proteins is a promising option for cancer treatment. However, current BET inhibitors are …
proteins is a promising option for cancer treatment. However, current BET inhibitors are …