[HTML][HTML] BET inhibitors: a novel epigenetic approach
DB Doroshow, JP Eder, PM LoRusso - Annals of Oncology, 2017 - Elsevier
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 …
Targeting bromodomains: epigenetic readers of lysine acetylation
P Filippakopoulos, S Knapp - Nature reviews Drug discovery, 2014 - nature.com
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 …
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 …
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 …
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 …
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 …
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 …
The BET bromodomain inhibitor OTX015 affects pathogenetic pathways in preclinical B-cell tumor models and synergizes with targeted drugs
Purpose: In cancer cells, the epigenome is often deregulated, and inhibition of the
bromodomain and extra-terminal (BET) family of bromodomain-containing proteins is a …
bromodomain and extra-terminal (BET) family of bromodomain-containing proteins is a …